Discovery of novel thieno[2,3-d]pyrimidin-4-yl hydrazone-based inhibitors of Cyclin D1-CDK4: Synthesis, biological evaluation and structure–activity relationships. Part 2
2009; Elsevier BV; Volume: 17; Issue: 23 Linguagem: Inglês
10.1016/j.bmc.2009.10.039
ISSN1464-3391
AutoresTakao Horiuchi, Motoko Nagata, Mayumi Kitagawa, Kouichi Akahane, Kouichi Uoto,
Tópico(s)Chronic Lymphocytic Leukemia Research
ResumoThe design, synthesis and evaluation of novel thieno[2,3-d]pyrimidin-4-yl hydrazone analogues as cyclin-dependent kinase 4 (CDK4) inhibitor are described. Focusing on the optimization of the heteroaryl moiety at the hydrazone with substituted phenyl groups, 4-[(methylamino)methyl]benzaldehyde (22) and 5-isoindolinecarbaldehyde (24) (6-tert-butylthieno[2,3-d]pyrimidin-4-yl)hydrazone derivatives have been identified. In this paper, the potency, selectivity profile and structure-activity relationships of our synthetic compounds are discussed.
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