Literature DB >> 17574416

Design, synthesis, and evaluation of 3,4-disubstituted pyrazole analogues as anti-tumor CDK inhibitors.

Ronghui Lin1, George Chiu, Yang Yu, Peter J Connolly, Shengjian Li, Yanhua Lu, Mary Adams, Angel R Fuentes-Pesquera, Stuart L Emanuel, Lee M Greenberger.   

Abstract

Two series of 3,4-disubstituted pyrazole analogues, 3-(benzimidazol-2-yl)-4-[2-(pyridin-3-yl)-vinyl]-pyrazoles (2) and 3-(imidazol-2-yl)-4-[2-(pyridin-3-yl)-vinyl]-pyrazoles (3), were synthesized as novel cyclin-dependent kinase (CDK) inhibitors. Representative compounds showed potent and selective CDK inhibitory activities and inhibited in vitro cellular proliferation in various human tumor cells. The design, synthesis, and preliminary biological evaluation of these pyrazole compounds are reported.

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Year:  2007        PMID： 17574416     DOI： 10.1016/j.bmcl.2007.05.092

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


  11 in total

1.  Efficient one-pot protocol for diverse pyrazolylphosphonates by multi-component reactions: their antioxidant and antibacterial activities.

Authors:  So Rang Kang; Yong Rok Lee
Journal:  Mol Divers       Date:  2015-02-05       Impact factor: 2.943

2.  Room temperature ICl-induced dehydration/iodination of 1-acyl-5-hydroxy-4,5-dihydro-1H-pyrazoles. a selective route to substituted 1-acyl-4-iodo-1H-pyrazoles.

Authors:  Jesse P Waldo; Saurabh Mehta; Richard C Larock
Journal:  J Org Chem       Date:  2008-07-30       Impact factor: 4.354

3.  Organometallic 3-(1H-benzimidazol-2-yl)-1H-pyrazolo[3,4-b]pyridines as potential anticancer agents.

Authors:  Iryna N Stepanenko; Maria S Novak; Gerhard Mühlgassner; Alexander Roller; Michaela Hejl; Vladimir B Arion; Michael A Jakupec; Bernhard K Keppler
Journal:  Inorg Chem       Date:  2011-10-27       Impact factor: 5.165

4.  Synthesis of 3,6-diaryl-1H-pyrazolo[3,4-b]pyridines via one-pot sequential Suzuki-Miyaura coupling.

Authors:  Vibha Tandon; Parthasarathi Das; S Kukreti
Journal:  RSC Adv       Date:  2018-10-11       Impact factor: 3.361

5.  Synthesis, characterization and anti-breast cancer activity of new 4-aminoantipyrine-based heterocycles.

Authors:  Mostafa M Ghorab; Marwa G El-Gazzar; Mansour S Alsaid
Journal:  Int J Mol Sci       Date:  2014-05-02       Impact factor: 5.923

6.  Molecular docking of 1H-pyrazole derivatives to receptor tyrosine kinase and protein kinase for screening potential inhibitors.

Authors:  Vishalakshi Gopalapura Javaregowda; Beeranahally Haruvegowda Doreswamy; Srikantamurthy Ningaiah; Umesha K Bhadraiah; Kempaiah Kemparaju; Mahendra Madegowda
Journal:  Bioinformation       Date:  2014-07-22

7.  Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy.

Authors:  Yogesh A Sonawane; Margaret A Taylor; John Victor Napoleon; Sandeep Rana; Jacob I Contreras; Amarnath Natarajan
Journal:  J Med Chem       Date:  2016-06-03       Impact factor: 7.446

8.  4-[5-(4-Chloro-phen-yl)-3-methyl-1H-pyrazol-1-yl]benzene-sulfonamide.

Authors:  Muhammad A Farrukh; Shaaban K Mohamed; Maqsood Ahmed; Adel A Marzouk; Samir M El-Moghazy
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2013-01-26

9.  Inhibitory effect of N-ethyl-3-amino-5-oxo-4-phenyl-2,5-dihydro-1H-pyrazole-1-carbothioamide on Haemophilus spp. planktonic or biofilm-forming cells.

Authors:  Urszula Kosikowska; Anna Malm; Monika Pitucha; Barbara Rajtar; Malgorzata Polz-Dacewicz
Journal:  Med Chem Res       Date:  2013-08-23       Impact factor: 1.965

10.  Synthesis of New 1,3,5-Triazine-Based 2-Pyrazolines as Potential Anticancer Agents.

Authors:  Leydi M Moreno; Jairo Quiroga; Rodrigo Abonia; Jonathan Ramírez-Prada; Braulio Insuasty
Journal:  Molecules       Date:  2018-08-06       Impact factor: 4.411
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