Literature DB >> 14552791

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

Concha Sanchez-Martinez1, Chuan Shih, Margaret M Faul, Guoxin Zhu, Michael Paal, Carmen Somoza, Tiechao Li, Christine A Kumrich, Leonard L Winneroski, Zhou Xun, Harold B Brooks, Bharvin K R Patel, Richard M Schultz, Tammy B DeHahn, Charles D Spencer, Scott A Watkins, Eileen Considine, Jack A Dempsey, Catherine A Ogg, Robert M Campbell, Bryan A Anderson, Jill Wagner.   

Abstract

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.

Entities:  

Mesh:

Substances:

Year:  2003        PMID: 14552791     DOI: 10.1016/s0960-894x(03)00791-1

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


  10 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.  Facile synthesis of indole- or benzofuran-fused benzo[a]carbazole-1,4-diones using a tandem two-step reaction sequence.

Authors:  Shanghui Tu; Chunyong Ding; Wenxiang Hu; Fulong Li; Qizheng Yao; Ao Zhang
Journal:  Mol Divers       Date:  2010-03-14       Impact factor: 2.943

3.  Testing the promiscuity of commercial kinase inhibitors against the AGC kinase group using a split-luciferase screen.

Authors:  Benjamin W Jester; Alicia Gaj; Carolyn D Shomin; Kurt J Cox; Indraneel Ghosh
Journal:  J Med Chem       Date:  2012-02-10       Impact factor: 7.446

4.  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 5.  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

6.  Kinase Inhibitor Screening Identifies Cyclin-Dependent Kinases and Glycogen Synthase Kinase 3 as Potential Modulators of TDP-43 Cytosolic Accumulation during Cell Stress.

Authors:  Diane Moujalled; Janine L James; Sarah J Parker; Grace E Lidgerwood; Clare Duncan; Jodi Meyerowitz; Takashi Nonaka; Masato Hasegawa; Katja M Kanninen; Alexandra Grubman; Jeffrey R Liddell; Peter J Crouch; Anthony R White
Journal:  PLoS One       Date:  2013-06-26       Impact factor: 3.240

7.  Ca(2+) permeable AMPA receptor induced long-term potentiation requires PI3/MAP kinases but not Ca/CaM-dependent kinase II.

Authors:  Suhail Asrar; Zikai Zhou; Wei Ren; Zhengping Jia
Journal:  PLoS One       Date:  2009-02-03       Impact factor: 3.240

8.  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

9.  Halogenation-Guided Chemical Screening Provides Insight into Tjipanazole Biosynthesis by the Cyanobacterium Fischerella ambigua.

Authors:  Tomasz Chilczuk; Till F Schäberle; Sahel Vahdati; Ute Mettal; Mustafa El Omari; Heike Enke; Michael Wiese; Gabriele M König; Timo H J Niedermeyer
Journal:  Chembiochem       Date:  2020-04-16       Impact factor: 3.164

10.  Antiamoebic Activities of Indolocarbazole Metabolites Isolated from Streptomyces sanyensis Cultures.

Authors:  Luis Cartuche; María Reyes-Batlle; Ines Sifaoui; Iñigo Arberas-Jiménez; José E Piñero; José J Fernández; Jacob Lorenzo-Morales; Ana R Díaz-Marrero
Journal:  Mar Drugs       Date:  2019-10-17       Impact factor: 5.118

  10 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.