1323138-80-2Relevant academic research and scientific papers
Synthesis and biological activities of 2-amino-thiazole-5-carboxylic acid phenylamide derivatives
Liu, Wukun,Zhou, Jinpei,Qi, Fan,Bensdorf, Kerstin,Li, Zhiyu,Zhang, Huibin,Qian, Hai,Huang, Wenlong,Cai, Xueting,Cao, Peng,Wellner, Anja,Gust, Ronald
, p. 451 - 458 (2012/02/01)
In an attempt to develop potent and selective anti-tumor drugs, a series of novel 2-amino-thiazole-5-carboxylic acid phenylamide derivatives were designed based on the structure of dasatinib. All compounds were synthesized by a systematic combinatorial chemical approach. Biological evaluation revealed that N-(2-chloro-6-methylphenyl)-2-(2-(4-methylpiperazin-1-yl)acetamido) thiazole-5-carboxamide (6d) exhibited high antiproliferative potency on human K563 leukemia cells comparable to dasatinib. Against mammary and colon carcinoma cells 6d was either inactive (MDA-MB 231) or distinctly less active (MCF-7 and HT-29: IC50=20.2 and 21.6μM, respectively). Dasatinib showed at each cell line IC501μM. The results of this structure activity relationship study clearly documented that the pyrimidin-4-ylamino core of dasatinib is responsible for the anti-tumor activity against non-leukemia cell lines.
Synthesis and cytotoxicity of novel 2-amino-5-thiazolecarboxamide derivatives
Li, Hu,Yue, Yun,Hu, Xiao-Jun,Zhao, Sheng-Yin
experimental part, p. 416 - 419 (2011/10/08)
A series of novel 2-amino-5-thiazolecarboxamide derivatives have been designed and synthesised. All the compounds were evaluated for their antiproliferative activity against human leukaemia cancer HL 60 and K562 cell lines by standard MTT assay in vitro. Some of these compounds showed moderate cytotoxic potencies. Structure-activity relationships suggested that the piperazine moiety in the side chain of 2-amino-5-thiazolecarboxamide was associated with an increase in the cytotoxicity.
