期刊
CHEMICAL & PHARMACEUTICAL BULLETIN
卷 59, 期 8, 页码 991-1002出版社
PHARMACEUTICAL SOC JAPAN
DOI: 10.1248/cpb.59.991
关键词
cyclin-dependent kinase 4 inhibitor; thieno[2,3-d]pyrimidine-4-yl hydrazone
The design, synthesis, and evaluation of novel thieno[2,3-d]pyrimidin-4-yl hydrazone analogues as cyclin-dependent kinase 4 (CDK4) inhibitors are described. In continuing our program aim to search for potent CDK4 inhibitors, the introduction of a thiazole group at the hydrazone part has led to marked enhancement of chemical stability. Furthermore, by focusing on the optimization at the C-4' position of the thiazole ring and the C-6 position of the thieno[2,3-d]pyrimidine moiety, compound 35 has been identified with efficacy in a xenograft model of HCT116 cells. In this paper, the potency, selectivity profile, and structure activity relationships of our synthetic compounds are discussed.
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