Literature DB >> 12657252

Synthesis of quinolinyl/isoquinolinyl[a]pyrrolo [3,4-c] carbazoles as cyclin D1/CDK4 inhibitors.

Guoxin Zhu1, Scott Conner, Xun Zhou, Chuan Shih, Harold B Brooks, Eileen Considine, Jack A Dempsey, Cathy Ogg, Bharvin Patel, Richard M Schultz, Charles D Spencer, Beverly Teicher, Scott A Watkins.   

Abstract

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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Year:  2003        PMID: 12657252     DOI: 10.1016/s0960-894x(03)00133-1

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  3 in total

1.  Synthesis and Initial in Vivo Studies with [(11)C]SB-216763: The First Radiolabeled Brain Penetrative Inhibitor of GSK-3.

Authors:  Lei Li; Xia Shao; Erin L Cole; Stephan A Ohnmacht; Valentina Ferrari; Young T Hong; David J Williamson; Tim D Fryer; Carole A Quesada; Phillip Sherman; Patrick J Riss; Peter J H Scott; Franklin I Aigbirhio
Journal:  ACS Med Chem Lett       Date:  2015-03-10       Impact factor: 4.345

2.  Effects of an Indolocarbazole-Derived CDK4 Inhibitor on Breast Cancer Cells.

Authors:  Yuan Sun; Ying-Xia Li; Hai-Jun Wu; Si-Hung Wu; Y Alan Wang; Dian-Zhong Luo; D Joshua Liao
Journal:  J Cancer       Date:  2011-01-08       Impact factor: 4.207

Review 3.  Marine pyrrolocarbazoles and analogues: synthesis and kinase inhibition.

Authors:  Sébastien Deslandes; Stefan Chassaing; Evelyne Delfourne
Journal:  Mar Drugs       Date:  2009-12-01       Impact factor: 5.118

  3 in total

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