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ChemInform Abstract: Covalent Modification of Cyclooxygenase-2 (COX-2) by 2-Acetoxyphenyl Alkyl Sulfides, a New Class of Selective COX-2 Inactivators.

✍ Scribed by Amit S. Kalgutkar; Kevin R. Kozak; Brenda C. Crews; G. Phillip Jr. Hochgesang; Lawrence J. Marnett

Publisher: John Wiley and Sons
Year: 2010
Weight: 32 KB
Volume: 30
Category: Article
ISSN: 0931-7597
DOI: 10.1002/chin.199913122

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✦ Synopsis

Covalent Modification of Cyclooxygenase-2 (COX-2) by 2-Acetoxyphenyl Alkyl Sulfides, a New Class of Selective COX-2 Inactivators.

-Structure-activity relationship investigation of a series of title compounds, e.g. (I)-(IV), shows that, besides compounds (IIb), (IIf), (IIg), and (IVa), the recently reported compound (IVb) displays the most potent and selective COX-2 in vivo inhibition by selective covalent modification. Thus, (IVb) can serve as therapeutic equivalent of aspirin in inflammatory and proliferative diseases (without the deleterious ulcerogenic side effects) and also as potential cancer chemopreventive agent, due to its ability to alternate growth of COX-2 expressing colon cancer cells. -(KALGUTKAR, AMIT S.;

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