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2‐Aminoxazole and 2‐Aminothiazole Dasatinib Derivatives as Potent Inhibitors of Chronic Myeloid Leukemia K562 Cells
Author(s) -
Chai XingXing,
Cai ZhiPing,
Yang MianTian,
Zhou Ying,
Fu YingJun,
Xiong YuanZhen
Publication year - 2016
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.201600010
Subject(s) - dasatinib , myeloid leukemia , imatinib , k562 cells , chemistry , pharmacology , chronic myelogenous leukemia , drug , leukemia , biological activity , cancer research , in vitro , medicine , biochemistry
Dasatinib is an important drug against chronic myeloid leukemia (CML). In this paper, we describe the preparation and anti‐CML activity of 2‐aminoxazole and 2‐aminothiazole dasatinib derivatives. Biological activity was measured by the inhibition of proliferation of human CML K562 cells. The 2‐aminoxazole derivatives had similar activities as the 2‐aminothiazole derivatives. All newly synthesized compounds demonstrated more potent antiproliferative activity than imatinib. A few compounds ( 8b , 8c , 9b ) showed nanomolar inhibitory activity, similar to that of dasatinib.