Literature DB >> 12824014

Novel, potent and selective cyclin D1/CDK4 inhibitors: indolo[6,7-a]pyrrolo[3,4-c]carbazoles.

Thomas A Engler1, Kelly Furness, Sushant Malhotra, Concha Sanchez-Martinez, Chuan Shih, Walter Xie, Guoxin Zhu, Xun Zhou, Scott Conner, Margaret M Faul, Kevin A Sullivan, Stanley P Kolis, Harold B Brooks, Bharvin Patel, Richard M Schultz, Tammy B DeHahn, Kashif Kirmani, Charles D Spencer, Scott A Watkins, Eileen L Considine, Jack A Dempsey, Catherine A Ogg, Nancy B Stamm, Bryan D Anderson, Robert M Campbell, Vasu Vasudevan, Michelle L Lytle.   

Abstract

The synthesis and CDK inhibitory properties of a series of indolo[6,7-a]pyrrolo[3,4-c]carbazoles is reported. In addition to their potent CDK activity, the compounds display antiproliferative activity against two human cancer cell lines. These inhibitors also effect strong G1 arrest in these cell lines and inhibit Rb phosphorylation at Ser780 consistent with inhibition of cyclin D1/CDK4.

Entities:  

Mesh:

Substances:

Year:  2003        PMID: 12824014     DOI: 10.1016/s0960-894x(03)00461-x

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


  4 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

4.  Arcyriaflavin a, a cyclin D1-cyclin-dependent kinase4 inhibitor, induces apoptosis and inhibits proliferation of human endometriotic stromal cells: a potential therapeutic agent in endometriosis.

Authors:  Tomoko Hirakawa; Kaei Nasu; Yoko Aoyagi; Kanetoshi Takebayashi; Hisashi Narahara
Journal:  Reprod Biol Endocrinol       Date:  2017-07-18       Impact factor: 5.211

  4 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.