- Discovery of 4-substituted methoxybenzoyl-aryl-thiazole as novel anticancer agents: Synthesis, biological evaluation, and structure-activity relationships
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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 μM 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.
- Lu, Yan,Li, Chien-Ming,Wang, Zhao,Ross, Charles R.,Chen, Jianjun,Dalton, James T.,Li, Wei,Miller, Duane D.
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experimental part
p. 1701 - 1711
(2010/01/16)
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- COMPOUNDS FOR TREATMENT OF CANCER
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Compounds according to formula (I) are disclosed where Q is S, N, or O; X is optional, and can be O═, S═, ═N—NH2, ═N—OH, or —OH; Y is optional and can be —N(H)—, O, or C1 to C20 hydrocarbon; and R1 and R2 are each independently substituted or unsubstituted single-, fused- or multiple-ring aryl or (hetero)cyclic ring systems. Methods of making these compounds, pharmaceutical compositions containing the compounds, and their use, particularly for treating or preventing cancer, are also disclosed.
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Page/Page column 18
(2010/01/31)
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