subject:(Sulphones)

Oregon State University

1. Kasperek, George James. The mechanism of some reactions of aryl α-disulfones.

Degree: PhD, Chemistry, 1969, Oregon State University

URL: http://hdl.handle.net/1957/45472

Subjects/Keywords: Sulphones

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APA (6^th Edition):

Kasperek, G. J. (1969). The mechanism of some reactions of aryl α-disulfones. (Doctoral Dissertation). Oregon State University. Retrieved from http://hdl.handle.net/1957/45472

Chicago Manual of Style (16^th Edition):

Kasperek, George James. “The mechanism of some reactions of aryl α-disulfones.” 1969. Doctoral Dissertation, Oregon State University. Accessed January 28, 2021. http://hdl.handle.net/1957/45472.

MLA Handbook (7^th Edition):

Kasperek, George James. “The mechanism of some reactions of aryl α-disulfones.” 1969. Web. 28 Jan 2021.

Vancouver:

Kasperek GJ. The mechanism of some reactions of aryl α-disulfones. [Internet] [Doctoral dissertation]. Oregon State University; 1969. [cited 2021 Jan 28]. Available from: http://hdl.handle.net/1957/45472.

Council of Science Editors:

Kasperek GJ. The mechanism of some reactions of aryl α-disulfones. [Doctoral Dissertation]. Oregon State University; 1969. Available from: http://hdl.handle.net/1957/45472

Oregon State University

2. Gabrielsen, Rolf Steven. The thermal decomposition of alkyl benzenediazo sulfones.

Degree: PhD, Chemistry, 1968, Oregon State University

URL: http://hdl.handle.net/1957/46490

Subjects/Keywords: Sulphones

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APA (6^th Edition):

Gabrielsen, R. S. (1968). The thermal decomposition of alkyl benzenediazo sulfones. (Doctoral Dissertation). Oregon State University. Retrieved from http://hdl.handle.net/1957/46490

Chicago Manual of Style (16^th Edition):

Gabrielsen, Rolf Steven. “The thermal decomposition of alkyl benzenediazo sulfones.” 1968. Doctoral Dissertation, Oregon State University. Accessed January 28, 2021. http://hdl.handle.net/1957/46490.

MLA Handbook (7^th Edition):

Gabrielsen, Rolf Steven. “The thermal decomposition of alkyl benzenediazo sulfones.” 1968. Web. 28 Jan 2021.

Vancouver:

Gabrielsen RS. The thermal decomposition of alkyl benzenediazo sulfones. [Internet] [Doctoral dissertation]. Oregon State University; 1968. [cited 2021 Jan 28]. Available from: http://hdl.handle.net/1957/46490.

Council of Science Editors:

Gabrielsen RS. The thermal decomposition of alkyl benzenediazo sulfones. [Doctoral Dissertation]. Oregon State University; 1968. Available from: http://hdl.handle.net/1957/46490

3. Penchalaiah, N. Organo sulphur and selenium compounds: synthesis, characterization, and biological evaluation of some (E) - and (Z)- sulphides, sulphones, sulphide-sulphones, di sulphones and some related selenium containing compounds; -.

Degree: Chemistry, 2012, Sri Krishnadevaraya University

URL: http://shodhganga.inflibnet.ac.in/handle/10603/5023

None

References given chapters wise

Advisors/Committee Members: Narayana Swamy, G.

Subjects/Keywords: sulphides; sulphones; sulphide-sulphones; di sulphones

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APA (6^th Edition):

Penchalaiah, N. (2012). Organo sulphur and selenium compounds: synthesis, characterization, and biological evaluation of some (E) - and (Z)- sulphides, sulphones, sulphide-sulphones, di sulphones and some related selenium containing compounds; -. (Thesis). Sri Krishnadevaraya University. Retrieved from http://shodhganga.inflibnet.ac.in/handle/10603/5023

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Chicago Manual of Style (16^th Edition):

Penchalaiah, N. “Organo sulphur and selenium compounds: synthesis, characterization, and biological evaluation of some (E) - and (Z)- sulphides, sulphones, sulphide-sulphones, di sulphones and some related selenium containing compounds; -.” 2012. Thesis, Sri Krishnadevaraya University. Accessed January 28, 2021. http://shodhganga.inflibnet.ac.in/handle/10603/5023.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

MLA Handbook (7^th Edition):

Penchalaiah, N. “Organo sulphur and selenium compounds: synthesis, characterization, and biological evaluation of some (E) - and (Z)- sulphides, sulphones, sulphide-sulphones, di sulphones and some related selenium containing compounds; -.” 2012. Web. 28 Jan 2021.

Vancouver:

Penchalaiah N. Organo sulphur and selenium compounds: synthesis, characterization, and biological evaluation of some (E) - and (Z)- sulphides, sulphones, sulphide-sulphones, di sulphones and some related selenium containing compounds; -. [Internet] [Thesis]. Sri Krishnadevaraya University; 2012. [cited 2021 Jan 28]. Available from: http://shodhganga.inflibnet.ac.in/handle/10603/5023.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Council of Science Editors:

Penchalaiah N. Organo sulphur and selenium compounds: synthesis, characterization, and biological evaluation of some (E) - and (Z)- sulphides, sulphones, sulphide-sulphones, di sulphones and some related selenium containing compounds; -. [Thesis]. Sri Krishnadevaraya University; 2012. Available from: http://shodhganga.inflibnet.ac.in/handle/10603/5023

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Hong Kong University of Science and Technology

4. Ng, Wai Man. Studies on DNA-cleaving agents : propargylic sulfones with sequence specificity.

Degree: 1998, Hong Kong University of Science and Technology

URL: http://repository.ust.hk/ir/Record/1783.1-3707 ; https://doi.org/10.14711/thesis-b603853 ; http://repository.ust.hk/ir/bitstream/1783.1-3707/1/th_redirect.html

► The purpose of this project is to determine the sequence specificity of novel propargylic sulfone compounds for DNA. Previous studies have shown that propargylic sulfones,… (more)

Subjects/Keywords: Antineoplastic agents ; Sulphones

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APA (6^th Edition):

Ng, W. M. (1998). Studies on DNA-cleaving agents : propargylic sulfones with sequence specificity. (Thesis). Hong Kong University of Science and Technology. Retrieved from http://repository.ust.hk/ir/Record/1783.1-3707 ; https://doi.org/10.14711/thesis-b603853 ; http://repository.ust.hk/ir/bitstream/1783.1-3707/1/th_redirect.html

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Chicago Manual of Style (16^th Edition):

Ng, Wai Man. “Studies on DNA-cleaving agents : propargylic sulfones with sequence specificity.” 1998. Thesis, Hong Kong University of Science and Technology. Accessed January 28, 2021. http://repository.ust.hk/ir/Record/1783.1-3707 ; https://doi.org/10.14711/thesis-b603853 ; http://repository.ust.hk/ir/bitstream/1783.1-3707/1/th_redirect.html.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

MLA Handbook (7^th Edition):

Ng, Wai Man. “Studies on DNA-cleaving agents : propargylic sulfones with sequence specificity.” 1998. Web. 28 Jan 2021.

Vancouver:

Ng WM. Studies on DNA-cleaving agents : propargylic sulfones with sequence specificity. [Internet] [Thesis]. Hong Kong University of Science and Technology; 1998. [cited 2021 Jan 28]. Available from: http://repository.ust.hk/ir/Record/1783.1-3707 ; https://doi.org/10.14711/thesis-b603853 ; http://repository.ust.hk/ir/bitstream/1783.1-3707/1/th_redirect.html.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Council of Science Editors:

Ng WM. Studies on DNA-cleaving agents : propargylic sulfones with sequence specificity. [Thesis]. Hong Kong University of Science and Technology; 1998. Available from: http://repository.ust.hk/ir/Record/1783.1-3707 ; https://doi.org/10.14711/thesis-b603853 ; http://repository.ust.hk/ir/bitstream/1783.1-3707/1/th_redirect.html

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Hong Kong University of Science and Technology

5. Lee, Yuk Ha. Studies on allylic rearrangement strategy to enediynes and intramolecular cyclization of hydroxyl propargylic sulfones.

Degree: 1999, Hong Kong University of Science and Technology

URL: http://repository.ust.hk/ir/Record/1783.1-1479 ; https://doi.org/10.14711/thesis-b641377 ; http://repository.ust.hk/ir/bitstream/1783.1-1479/1/th_redirect.html

► Enediyne natural products are among the most potent antitumor agents known today. Numerous synthetic methodologies for the synthesis of naturally occurring enediynes and their analogs… (more)

▼ Enediyne natural products are among the most potent antitumor agents known today. Numerous synthetic methodologies for the synthesis of naturally occurring enediynes and their analogs have been developed over the last decade. Ally lit rearrangement first reported by our group is one of such methods that allow formation of the labile enediyne moiety from a stable precursor. This thesis study will emphasize on the study of allylic rearrangement of 1,2-dialkynylallyl alcohols and esters under protic or Lewis acid catalysis. A minor effort will be devoted to the study of β-hydroxyl propargylic sulfones, the well-known DNA base alkylating agents. An overview of the naturally occurring enediyne family including selected synthetic approaches to their model systems is outlined in Chapter 1. In Chapter 2, selected methodologies for the formation of enediynes from 1,5-diynes are reviewed followed by a background description on the allylic rearrangement strategy. A detailed account on the mechanism, regio- and diastereoselectivity of the protic acid-catalyzed rearrangement of 1,2-dialkynylallyl alcohols is then provided on the basis of new results of this thesis study. They include: (a) examination of structural requirement for facile rearrangement; (b) reactions using chiral ally1 alcohols to probe the reactive intermediates involved in the product-forming step; (c) computational calculations on the stability of substrates, products and the allylic cations for the understanding of substrate reactivity, regio- and diastereoselectivity. Chapter 3 deals with the control of regiochemistry in the protic acid-catalyzed allylic rearrangement. C3-aryl ally1 alcohols possessing an internal nucleophilic site (hydroxymethyl or mercarptomethyl group) are synthesized. Protic acid-catalyzed rearrangement of these substrates is shown to give the desired cis-enediynes in a complete regiocontrolled manner. A novel Eu(fod)3-catalyzed rearrangement of allylic esters is presented in Chapter 4. In this study, the reactivity of a number of allylic esters is examined systematically. We find that esters having an additional chelating site are capable of forming a five- or six-membered chelate with Eu(III) and migrate readily at room temperature. Among them, allylic methoxyacetates and benzyloxyacetates are the choices of esters and a number of enediynes can be prepared by this mild rearrangement. The final chapter investigates the base-catalyzed cyclization of a series of β-hydroxyl propargylic sulfones to form (E)-exe-alkylidene tetrahydrofurans. The mechanism is established using the deuterium-trapping experiment. On the basis of these results, the diminished DNA cleaving potency of these β-hydroxyl propargylic sulfones compared to the corresponding acetates is understood and is attributed to the self-cyclization to form (E)-exe-alkylidene tetrahydrofurans.

Subjects/Keywords: Antineoplastic agents – Synthesis ; Esters ; Sulphones

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APA · Chicago · MLA · Vancouver · CSE | Export to Zotero / EndNote / Reference Manager

APA (6^th Edition):

Lee, Y. H. (1999). Studies on allylic rearrangement strategy to enediynes and intramolecular cyclization of hydroxyl propargylic sulfones. (Thesis). Hong Kong University of Science and Technology. Retrieved from http://repository.ust.hk/ir/Record/1783.1-1479 ; https://doi.org/10.14711/thesis-b641377 ; http://repository.ust.hk/ir/bitstream/1783.1-1479/1/th_redirect.html

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Chicago Manual of Style (16^th Edition):

Lee, Yuk Ha. “Studies on allylic rearrangement strategy to enediynes and intramolecular cyclization of hydroxyl propargylic sulfones.” 1999. Thesis, Hong Kong University of Science and Technology. Accessed January 28, 2021. http://repository.ust.hk/ir/Record/1783.1-1479 ; https://doi.org/10.14711/thesis-b641377 ; http://repository.ust.hk/ir/bitstream/1783.1-1479/1/th_redirect.html.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

MLA Handbook (7^th Edition):

Lee, Yuk Ha. “Studies on allylic rearrangement strategy to enediynes and intramolecular cyclization of hydroxyl propargylic sulfones.” 1999. Web. 28 Jan 2021.

Vancouver:

Lee YH. Studies on allylic rearrangement strategy to enediynes and intramolecular cyclization of hydroxyl propargylic sulfones. [Internet] [Thesis]. Hong Kong University of Science and Technology; 1999. [cited 2021 Jan 28]. Available from: http://repository.ust.hk/ir/Record/1783.1-1479 ; https://doi.org/10.14711/thesis-b641377 ; http://repository.ust.hk/ir/bitstream/1783.1-1479/1/th_redirect.html.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Council of Science Editors:

Lee YH. Studies on allylic rearrangement strategy to enediynes and intramolecular cyclization of hydroxyl propargylic sulfones. [Thesis]. Hong Kong University of Science and Technology; 1999. Available from: http://repository.ust.hk/ir/Record/1783.1-1479 ; https://doi.org/10.14711/thesis-b641377 ; http://repository.ust.hk/ir/bitstream/1783.1-1479/1/th_redirect.html

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Hong Kong University of Science and Technology

6. Lor, Sze Keung. Second harmonic nonlinear optical properties of disperse red 1 loaded polysulfones.

Degree: 1996, Hong Kong University of Science and Technology

URL: http://repository.ust.hk/ir/Record/1783.1-1472 ; https://doi.org/10.14711/thesis-b502074 ; http://repository.ust.hk/ir/bitstream/1783.1-1472/1/th_redirect.html

► Two approaches were employed to prepare polymeric materials for studying second order nonlinear effects, particularly second harmonic generation (SHG) in polysulfones. The first approach is… (more)

Subjects/Keywords: Protective coatings – Optical properties ; Nonlinear optics ; Sulphones

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APA (6^th Edition):

Lor, S. K. (1996). Second harmonic nonlinear optical properties of disperse red 1 loaded polysulfones. (Thesis). Hong Kong University of Science and Technology. Retrieved from http://repository.ust.hk/ir/Record/1783.1-1472 ; https://doi.org/10.14711/thesis-b502074 ; http://repository.ust.hk/ir/bitstream/1783.1-1472/1/th_redirect.html

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Chicago Manual of Style (16^th Edition):

Lor, Sze Keung. “Second harmonic nonlinear optical properties of disperse red 1 loaded polysulfones.” 1996. Thesis, Hong Kong University of Science and Technology. Accessed January 28, 2021. http://repository.ust.hk/ir/Record/1783.1-1472 ; https://doi.org/10.14711/thesis-b502074 ; http://repository.ust.hk/ir/bitstream/1783.1-1472/1/th_redirect.html.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

MLA Handbook (7^th Edition):

Lor, Sze Keung. “Second harmonic nonlinear optical properties of disperse red 1 loaded polysulfones.” 1996. Web. 28 Jan 2021.

Vancouver:

Lor SK. Second harmonic nonlinear optical properties of disperse red 1 loaded polysulfones. [Internet] [Thesis]. Hong Kong University of Science and Technology; 1996. [cited 2021 Jan 28]. Available from: http://repository.ust.hk/ir/Record/1783.1-1472 ; https://doi.org/10.14711/thesis-b502074 ; http://repository.ust.hk/ir/bitstream/1783.1-1472/1/th_redirect.html.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Council of Science Editors:

Lor SK. Second harmonic nonlinear optical properties of disperse red 1 loaded polysulfones. [Thesis]. Hong Kong University of Science and Technology; 1996. Available from: http://repository.ust.hk/ir/Record/1783.1-1472 ; https://doi.org/10.14711/thesis-b502074 ; http://repository.ust.hk/ir/bitstream/1783.1-1472/1/th_redirect.html

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Hong Kong University of Science and Technology

7. Chow, Chun Wo. Synthesis and DNA cleavage of phenyl and 2-naphthyl propargylic sulfones and study on axially chiral 2-substituted N,N-dialkyl-1-naphthamides.

Degree: 2000, Hong Kong University of Science and Technology

URL: http://repository.ust.hk/ir/Record/1783.1-4003 ; https://doi.org/10.14711/thesis-b673091 ; http://repository.ust.hk/ir/bitstream/1783.1-4003/1/th_redirect.html

► In this thesis work, two classes of compounds are studied. They are the phenyl and 2-naphthyl propargylic sulfones used as DNA cleaving agents, and the… (more)

▼ In this thesis work, two classes of compounds are studied. They are the phenyl and 2-naphthyl propargylic sulfones used as DNA cleaving agents, and the axially chiral 2-substituted N,N-dialkyl-1-naphthamides. The first part of the thesis consists of two chapters. After a brief overview of the anticancer agents in Chapter One, Chapter Two deals with the synthesis and biological studies of novel propargylic sulfones. Propargylic sulfones are known to readily isomerize into allenic sulfones under mild basic conditions. The latter substances are highly electrophilic and react with nucleic bases to produce base-alkylated DNA, an event leading to DNA strand breakage and cell death. Mechanistic studies by other groups reveal that propargylic sulfones preferably attack at G residues and show clear sequence specificities. Recent reports from this group demonstrate that incorporation of DNA intercalators into the phenyl propargylic sulfone conjugates significantly enhances the DNA cleavage potency. In this thesis work, the author synthesized a series of phenyl propargylic sulfone conjugates possessing a short spacer group between the sulfone and the intercalator and observed the effect of the spacer group on the action of the conjugates. In parallel, a novel series of 2-naphthyl propargylic sulfones and conjugates were designed and synthesized in the hope that the 2-naphthyl group can serve for both DNA alkylation and intercalation. Experimental results confirmed that the 2-naphthyl propargylic sulfones with a free hydroxyl group are highly potent DNA cleavers that produce >80% net strand cut at 100 μM. The corresponding aromatic ester conjugates, however, showed a reduced DNA cleavage potency in contrast to the observation on the phenyl propargylic sulfones. Cytotoxicity of the 2-naphthyl propargylic sulfones against P388 mouse T cell leukemia was assayed and the conjugates possessing a short spacer group are more potent than the analogs having additional one or two methylene unit(s) in the spacer. 2-Substituted N,N-dialkyl-1-naphthamides are chiral due to the restricted rotation around the Ar-C(O)N single bond. Chapter Three of the thesis describes some preliminary results on the separation of these enantiomerically pure atropoisomers by HPLC over a chiral stationary phase (Chiralpak AD). Although the absolute stereochemistry of the separated axially chiral amides has not been determined, they were used as the chiral promoters in the catalytic enantioselective ethylation of benzaldehyde with diethylzinc. Asymmetric induction was observed to some extent, though it is not satisfactory compared with the existing available methodologies. Nevertheless, these preliminary results are of reference value for future development on this emerging topic of axially chiral molecules.

Subjects/Keywords: DNA-drug interactions ; Antineoplastic antibiotics – Synthesis ; Sulphones – Synthesis ; Amides ; Chirality

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APA (6^th Edition):

Chow, C. W. (2000). Synthesis and DNA cleavage of phenyl and 2-naphthyl propargylic sulfones and study on axially chiral 2-substituted N,N-dialkyl-1-naphthamides. (Thesis). Hong Kong University of Science and Technology. Retrieved from http://repository.ust.hk/ir/Record/1783.1-4003 ; https://doi.org/10.14711/thesis-b673091 ; http://repository.ust.hk/ir/bitstream/1783.1-4003/1/th_redirect.html

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Chicago Manual of Style (16^th Edition):

Chow, Chun Wo. “Synthesis and DNA cleavage of phenyl and 2-naphthyl propargylic sulfones and study on axially chiral 2-substituted N,N-dialkyl-1-naphthamides.” 2000. Thesis, Hong Kong University of Science and Technology. Accessed January 28, 2021. http://repository.ust.hk/ir/Record/1783.1-4003 ; https://doi.org/10.14711/thesis-b673091 ; http://repository.ust.hk/ir/bitstream/1783.1-4003/1/th_redirect.html.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

MLA Handbook (7^th Edition):

Chow, Chun Wo. “Synthesis and DNA cleavage of phenyl and 2-naphthyl propargylic sulfones and study on axially chiral 2-substituted N,N-dialkyl-1-naphthamides.” 2000. Web. 28 Jan 2021.

Vancouver:

Chow CW. Synthesis and DNA cleavage of phenyl and 2-naphthyl propargylic sulfones and study on axially chiral 2-substituted N,N-dialkyl-1-naphthamides. [Internet] [Thesis]. Hong Kong University of Science and Technology; 2000. [cited 2021 Jan 28]. Available from: http://repository.ust.hk/ir/Record/1783.1-4003 ; https://doi.org/10.14711/thesis-b673091 ; http://repository.ust.hk/ir/bitstream/1783.1-4003/1/th_redirect.html.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Council of Science Editors:

Chow CW. Synthesis and DNA cleavage of phenyl and 2-naphthyl propargylic sulfones and study on axially chiral 2-substituted N,N-dialkyl-1-naphthamides. [Thesis]. Hong Kong University of Science and Technology; 2000. Available from: http://repository.ust.hk/ir/Record/1783.1-4003 ; https://doi.org/10.14711/thesis-b673091 ; http://repository.ust.hk/ir/bitstream/1783.1-4003/1/th_redirect.html

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

University of Florida

8. Price, George Dodds, 1928-. Theoretical studies on unsaturated compounds containing sulfur.

Degree: 1964, University of Florida

URL: https://ufdc.ufl.edu/AA00047108

Subjects/Keywords: Anhydrides; Copyrights; Dioxanes; Hydrogen; Molecular weight; Monomers; Polymers; Sulfides; Sulfones; Wavelengths; Chemistry thesis Ph. D; Polymers and polymerization; Sulphones

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APA (6^th Edition):

Price, George Dodds, 1. (1964). Theoretical studies on unsaturated compounds containing sulfur. (Thesis). University of Florida. Retrieved from https://ufdc.ufl.edu/AA00047108

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Chicago Manual of Style (16^th Edition):

Price, George Dodds, 1928-. “Theoretical studies on unsaturated compounds containing sulfur.” 1964. Thesis, University of Florida. Accessed January 28, 2021. https://ufdc.ufl.edu/AA00047108.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

MLA Handbook (7^th Edition):

Price, George Dodds, 1928-. “Theoretical studies on unsaturated compounds containing sulfur.” 1964. Web. 28 Jan 2021.

Vancouver:

Price, George Dodds 1. Theoretical studies on unsaturated compounds containing sulfur. [Internet] [Thesis]. University of Florida; 1964. [cited 2021 Jan 28]. Available from: https://ufdc.ufl.edu/AA00047108.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Council of Science Editors:

Price, George Dodds 1. Theoretical studies on unsaturated compounds containing sulfur. [Thesis]. University of Florida; 1964. Available from: https://ufdc.ufl.edu/AA00047108

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Georgia Tech

9. Gotz, Marion Gabriele. Design, synthesis, and evaluation of irreversible peptidyl inhibitors for clan CA and clan CD cysteine proteases.

Degree: PhD, Chemistry and Biochemistry, 2004, Georgia Tech

URL: http://hdl.handle.net/1853/8072

► Cysteine proteases are a class of proteolytic enzymes, which are involved in a series of metabolic and catabolic processes, such as protein turnover, digestion, blood… (more)

▼ Cysteine proteases are a class of proteolytic enzymes, which are involved in a series of metabolic and catabolic processes, such as protein turnover, digestion, blood coagulation, apoptosis, fertilization and cell differentiation, and the immune response system. The development of novel potent and selective inhibitors for cysteine proteases has therefore gained increasing attention among medicinal chemists. In this thesis we have reported the design, synthesis, and evaluation of several peptidyl inhibitors for clan CA and clan CD cysteine proteases. We have continued the investigation of dipeptidyl vinyl sulfones as potent and selective inhibitors for dipeptidyl peptidase I (DPPI), a lysosomal cysteine protease, which is involved in the processing of intracellular proteases, such as granzymes. We have found that DPPI tolerates negatively charged amino acid residues in the P2 position with inhibition rates of 7,600 M-1s-1. Dipeptidyl vinyl sulfones with positively charged amino acid residues at the P1 position, however, do not inhibit DPPI at all. A second project focused on the epoxidation of the double bond of the vinyl sulfone moiety of the dipeptidyl vinyl sulfones. Instead of epoxidizing the double bond, we found that an isomerization had occurred. The newly formed compounds were determined to be allyl sulfones. We tested this new class of inhibitors with clan CA proteases and obtained inhibition rates of 560 M-1s-1 for Cbz-Leu-Phe-AS-Ph with calpain I. Two new classes of compounds for the clan CD protease S. mansoni legumain were designed, synthesized, and evaluated. Aza-peptidyl epoxides were found to be potent and selective inhibitors of S. mansoni legumain with IC50’s as low as 45 nM. Aza-peptide Michael acceptors were derived from the aza-peptide epoxide design and synthesized in an analogous fashion. The aza-peptide Michael acceptors inhibited S. mansoni legumain with even lower IC50’s, as low as 10 nM. However, the aza-peptide Michael acceptors react with thioalkylating agents contained in the buffer, such as DTT. The rates of degradation were determined spectroscopically, and half-lives of 3 to 20 minutes were measured. This observation gave us insights into the enzymatic mechanism and allowed us to determine the point of attack for the legumain active site cysteine thiol. Advisors/Committee Members: Dr. James C. Powers (Committee Chair), Dr. Donald Doyle, Dr. Nicholas Hud, Dr. Niren Murthy, and Dr. Suzanne Shuker (Committee Members).

Subjects/Keywords: Allyl sulfone; Aza-peptide; Biosynthesis; Cysteine protease; Cysteine proteinases; Irreversible inhibitors; Protease inhibitors; Sulphones; Vinyl sulfone

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APA (6^th Edition):

Gotz, M. G. (2004). Design, synthesis, and evaluation of irreversible peptidyl inhibitors for clan CA and clan CD cysteine proteases. (Doctoral Dissertation). Georgia Tech. Retrieved from http://hdl.handle.net/1853/8072

Chicago Manual of Style (16^th Edition):

Gotz, Marion Gabriele. “Design, synthesis, and evaluation of irreversible peptidyl inhibitors for clan CA and clan CD cysteine proteases.” 2004. Doctoral Dissertation, Georgia Tech. Accessed January 28, 2021. http://hdl.handle.net/1853/8072.

MLA Handbook (7^th Edition):

Gotz, Marion Gabriele. “Design, synthesis, and evaluation of irreversible peptidyl inhibitors for clan CA and clan CD cysteine proteases.” 2004. Web. 28 Jan 2021.

Vancouver:

Gotz MG. Design, synthesis, and evaluation of irreversible peptidyl inhibitors for clan CA and clan CD cysteine proteases. [Internet] [Doctoral dissertation]. Georgia Tech; 2004. [cited 2021 Jan 28]. Available from: http://hdl.handle.net/1853/8072.

Council of Science Editors:

Gotz MG. Design, synthesis, and evaluation of irreversible peptidyl inhibitors for clan CA and clan CD cysteine proteases. [Doctoral Dissertation]. Georgia Tech; 2004. Available from: http://hdl.handle.net/1853/8072

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Open Access Theses and Dissertations