Synthesis of quinolinyl/isoquinolinyl[a]pyrrolo [3,4-c] carbazoles as cyclin D1/CDK4 inhibitors.
作者信息
Zhu Guoxin, Conner Scott, Zhou Xun, Shih Chuan, Brooks Harold B, Considine Eileen, Dempsey Jack A, Ogg Cathy, Patel Bharvin, Schultz Richard M, Spencer Charles D, Teicher Beverly, Watkins Scott A
机构信息
Lilly Research Laboratories, A Division of Eli Lilly and Company, Lilly Corporate Center, Indianapolis, IN 46285, USA.
出版信息
Bioorg Med Chem Lett. 2003 Apr 7;13(7):1231-5. doi: 10.1016/s0960-894x(03)00133-1.
A novel series of pyrrolo[3,4-c] carbazoles fused with a quinolinyl/isoquinolinyl moiety were synthesized and their D1/CDK4 inhibitory and antiproliferative activity were evaluated. Compound 8H, 14H-isoquinolinyl[6,5-a]-pyrrolo[3,4-c]carbazole-7,9-dione (1d) was found to be a highly potent D1/CDK4 inhibitor with an IC(50) of 69 nM. Compound 1d also inhibited tumor cell growth, arrested tumor cells in G1 phase and inhibited pRb phosphorylation.
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