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Your search keyword '"Li, Chien-Ming"' showing total 6 results
Start Over Author "Li, Chien-Ming" Journal journal of medicinal chemistry
6 results on '"Li, Chien-Ming"'

6. Discovery of 4-substituted methoxybenzoyl-aryl-thiazole as novel anticancer agents: synthesis, biological evaluation, and structure-activity relationships.

Author

Lu Y, Li CM, Wang Z, Ross CR 2nd, Chen J, Dalton JT, Li W, and Miller DD

Subjects
Antineoplastic Agents chemical synthesis, Drug Screening Assays, Antitumor, Humans, Magnetic Resonance Spectroscopy, Male, Structure-Activity Relationship, Thiazoles chemical synthesis, Antineoplastic Agents chemistry, Antineoplastic Agents pharmacology, Thiazoles chemistry, Thiazoles pharmacology
Abstract

A series of 4-substituted methoxybenzoyl-aryl-thiazoles (SMART) have been discovered and synthesized as a result of structural modifications of the lead compound 2-arylthiazolidine-4-carboxylic acid amides (ATCAA). The antiproliferative activity of the SMART agents against melanoma and prostate cancer cells was improved from muM to low nM range compared with the ATCAA series. The structure-activity relationship was discussed from modifications of "A", "B", and "C" rings and the linker. Preliminary mechanism of action studies indicated that these compounds exert their anticancer activity through inhibition of tubulin polymerization.

Published
2009
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