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Design, Synthesis and Antiproliferative Activity of 2-Acetamidothiazole-5- carboxamide Derivatives

[ Vol. 8 , Issue. 4 ]


Wukun Liu, Jinpei Zhou, Yu Zheng, Fan Qi, Huibin Zhang, Hai Qian, Jing Wang, Yanhua Cheng and Ronald Gust   Pages 587 - 594 ( 8 )


In order to develop a new series of dual inhibitors of SRC and ABL, and to investigate whether the pyrimidin- 4-ylamino moiety is critical for dasatinib’s activity, acetyl substitution was adopted as alternate scaffold at the 2-amino group. Eighteen novel dasatinib derivatives were developed by a parallel synthesis approach and evaluated for their antiproliferative effects. Preliminary tests showed that some of the target compounds IId, IIe and IIf manifested strong antiproliferative activity against MCF-7, MDA-MB 231 and HT-29 cells. Easpecially IId proved to be the most potent compound. Structure-activity relationship studies indicate that the introduction of acetyl substitution as alternate scaffold of pyrimidin-4-ylamino reduced the activity.


Dasatinib, Antiproliferative Activity, SRC Kinase Inhibitor, Synthesis, Structure-Activity Relationship Studies, pyrimidin-4-ylamino, MDA-MB 231, HT-29 cells, ABL kinase, chronic myeloid leukaemia


Department of Math and Computer, Nanjing Medical University, 140 Hanzhonglu, Nanjing 210029, China.

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