title: 2-Aminoxazole and 2-Aminothiazole Dasatinib Derivatives as Potent Inhibitors of Chronic Myeloid Leukemia K562 Cells.
abstract: 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.
authors.affiliation: Medical School of Nanchang University, Nanchang, China.
authors.forename: Xing-Xing
authors.initials: XX
authors.lastname: Chai
authors.affiliation: Medical School of Nanchang University, Nanchang, China.
authors.forename: Zhi-Ping
authors.initials: ZP
authors.lastname: Cai
authors.affiliation: Medical School of Nanchang University, Nanchang, China.
authors.forename: Mian-Tian
authors.initials: MT
authors.lastname: Yang
authors.affiliation: Medical School of Nanchang University, Nanchang, China.
authors.forename: Ying
authors.initials: Y
authors.lastname: Zhou
authors.affiliation: Medical School of Nanchang University, Nanchang, China.
authors.forename: Ying-Jun
authors.initials: YJ
authors.lastname: Fu
authors.affiliation: Medical School of Nanchang University, Nanchang, China.
authors.forename: Yuan-Zhen
authors.initials: YZ
authors.lastname: Xiong
mesh_terms: D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D000069439:Dasatinib / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology*; D006801:Humans; D015464:Leukemia, Myelogenous, Chronic, BCR-ABL Positive / Q000473:pathology*; D010080:Oxazoles / Q000138:chemical synthesis / Q000494:pharmacology; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000138:chemical synthesis / Q000494:pharmacology
chemical_list: D010080:Oxazoles; D013844:Thiazoles; D000069439:Dasatinib
keywords: 2-aminothiazole series; 2-aminoxazole series; CML inhibitor; Dasatinib derivatives