Cyanopyridyl containing 1, 4-dihydroindeno [1, 2-c] pyrazoles as potent checkpoint kinase 1 inhibitors: Improving oral biovailability

…, M Przytulinska, ZF Tao, J Bouska, KD Stewart…

文献索引：Tong, Yunsong; Przytulinska, Magdalena; Tao, Zhi-Fu; Bouska, Jennifer; Stewart, Kent D.; Park, Chang; Li, Gaoquan; Claiborne, Akiyo; Kovar, Peter; Chen, Zehan; Merta, Philip J.; Bui, Mai-Ha; Olson, Amanda; Osterling, Donald; Zhang, Haiying; Sham, Hing L.; Rosenberg, Saul H.; Sowin, Thomas J.; Lin, Nan-horng Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 20 p. 5665 - 5670

全文：HTML全文

被引用次数: 5

摘要

A series of 1, 4-dihydroindeno [1, 2-c] pyrazole compounds with a cyanopyridine moiety at the 3-position of the tricyclic pyrazole core was explored as potent CHK-1 inhibitors. The impact of substitutions at the 6 and/or 7-position of the core on pharmacokinetic properties was studied in detail. Compounds carrying a side chain with an ether linker at the 7-position and a terminal morpholino group, such as 29 and 30, exhibited much-improved oral ...