106086-10-6Relevant articles and documents
Stereoselective synthesis of chiral thiol-containing 1,2-aminoalcohols via SmI2-mediated coupling
Doler, Carina,Friess, Michael,Lackner, Florian,Weber, Hansj?rg,Fischer, Roland C.,Breinbauer, Rolf
, (2020/05/14)
The stereoselective synthesis of highly functionalized aminohydroxythiols represents a synthetic challenge as the oxidation sensitivity and coordinating property of the thiol group interferes with many established synthetic methods. The SmI2/Li
Synthesis, in vitro structure-activity relationship, and in vivo studies of 2-arylthiazolidine-4-carboxylic acid amides as anticancer agents
Lu, Yan,Wang, Zhao,Li, Chien-Ming,Chen, Jianjun,Dalton, James T.,Li, Wei,Miller, Duane D.
experimental part, p. 477 - 495 (2010/04/29)
A series of (2RS,4R)-2-arylthiazolidine-4-carboxylic acid amide (ATCAA) was synthesized. Antiproliferative activity against melanoma and prostate cancer cells compared with control cells (fibroblast and RH7777, respectively) was evaluated. Compound 3id sh
Discovery of 4-substituted methoxybenzoyl-aryl-thiazole as novel anticancer agents: Synthesis, biological evaluation, and structure-activity relationships
Lu, Yan,Li, Chien-Ming,Wang, Zhao,Ross, Charles R.,Chen, Jianjun,Dalton, James T.,Li, Wei,Miller, Duane D.
experimental part, p. 1701 - 1711 (2010/01/16)
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.