Aryl[a]pyrrolo[3,4-c]carbazoles as selective cyclin D1-CDK4 inhibitors.

  title={Aryl[a]pyrrolo[3,4-c]carbazoles as selective cyclin D1-CDK4 inhibitors.},
  author={Concha S{\'a}nchez-Mart{\'i}nez and C -Y.T. Shih and M. Faul and Guoxin Zhu and Michael Paal and Carmen Somoza and Tiechao Li and Christine A Kumrich and Leonard L. Winneroski and Zhou Xun and Harold B. Brooks and Bharvin K.R. Patel and Richard M Schultz and Tammy B DeHahn and Charles D Spencer and Scott A Watkins and Eileen L. Considine and Jack Alan Dempsey and Catherine A Ogg and Robert Morris Campbell and B. A. Anderson and Jill R Wagner},
  journal={Bioorganic & medicinal chemistry letters},
  volume={13 21},
The synthesis of new analogues of Arcyriaflavin A in which one indole ring is replaced by an aryl or heteroaryl ring is described. These new series of aryl[a]pyrrolo[3,4-c]carbazoles were evaluated as inhibitors of Cyclin D1-CDK4. A potent and selective D1-CDK4 inhibitor, 7a (D1-CDK4 IC(50)=45 nM), has been identified. The potency, selectivity profile against other kinases, and structure-activity relationship (SAR) trends of this class of compounds are discussed. 
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