Discovery of 4-substituted methoxybenzoyl-aryl-thiazole as novel anticancer agents: synthesis, biological evaluation, and structure-activity relationships.
Discovery of 4-substituted methoxybenzoyl-aryl-thiazole as novel anticancer agents: synthesis, biological evaluation, and structure-activity relationships.
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DOI：
10.1021/jm801449a
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发表时间：
2009-03-26
影响因子：
7.3
通讯作者：
Miller DD
中科院分区：
文献类型：
--
作者：
Lu Y;Li CM;Wang Z;Ross CR 2nd;Chen J;Dalton JT;Li W;Miller DD
通过对先导化合物 2-芳基噻唑烷-4-甲酰胺 (ATCAA) 进行结构修饰，人们发现并合成了一系列 4-取代的甲氧基苯甲酰基-芳基-噻唑 (SMART)。与ATCAA系列相比，SMART药物对黑色素瘤和前列腺癌细胞的抗增殖活性从μM提高到低nM范围。从“A”、“B”、“C”环和连接体的修饰讨论构效关系。初步作用机制研究表明，这些化合物通过抑制微管蛋白聚合发挥抗癌活性。
A series of 4-substituted methoxylbenzoyl-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 ATCAA series. The structure-activity relationship was discussed from modifications of “A”, “B” “C” rings and the linker. Preliminary mechanism of action studies indicated that these compounds exert their anticancer activity through inhibition of tubulin polymerization.
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影响因子：
4.8
作者：
Guo, Rishu;Kasbohm, Elizabeth A.;Daaka, Yehia
通讯作者：
Daaka, Yehia
DOI：
10.1073/pnas.74.8.3466
发表时间：
1977-01-01
影响因子：
11.1
作者：
MARGOLIS, RL;WILSON, L
通讯作者：
WILSON, L
影响因子：
15
作者：
PRATT, YT;DRAKE, NL
通讯作者：
DRAKE, NL
影响因子：
1.8
作者：
NAHM, S;WEINREB, SM
通讯作者：
WEINREB, SM
DOI：
10.1039/j39680001526
发表时间：
1968-01-01
期刊：
JOURNAL OF THE CHEMICAL SOCIETY C-ORGANIC
影响因子：
--
作者：
FULLER, NA;WALKER, J
通讯作者：
WALKER, J