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Imidazo [1, 2-b] pyridazines: a potent and selective class of cyclin-dependent kinase inhibitors

…, J Breed, A Pannifer, S Rowsell, JJ Stanway…

文献索引:Byth, Kate F.; Cooper, Nicola; Culshaw, Janet D.; Heaton, David W.; Oakes, Sandra E.; Minshull, Claire A.; Norman, Richard A.; Pauptit, Richard A.; Tucker, Julie A.; Breed, Jason; Pannifer, Andrew; Rowsell, Sian; Stanway, Judith J.; Valentine, Anna L.; Thomas, Andrew P. Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 9 p. 2249 - 2252

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被引用次数: 61

摘要

Modification of imidazo [1, 2-a] pyridine CDK inhibitors lead to identification of less lipophilic imidazo [1, 2-b] pyridazine series of CDK inhibitors. Although several equivalent compounds from these two series have similar structure and show similar CDK activity, the SAR of the two series differs significantly. Protein inhibitor structure determination has confirmed differences in binding mode and given some understanding of these differences in SAR. ...