Literature DB >> 17904841

Pyrazolo[1,5-a]pyrimidines as orally available inhibitors of cyclin-dependent kinase 2.

Kamil Paruch1, Michael P Dwyer, Carmen Alvarez, Courtney Brown, Tin-Yau Chan, Ronald J Doll, Kerry Keertikar, Chad Knutson, Brian McKittrick, Jocelyn Rivera, Randall Rossman, Greg Tucker, Thierry O Fischmann, Alan Hruza, Vincent Madison, Amin A Nomeir, Yaolin Wang, Emma Lees, David Parry, Nicole Sgambellone, Wolfgang Seghezzi, Lesley Schultz, Fran Shanahan, Derek Wiswell, Xiaoying Xu, Quiao Zhou, Ray A James, Vidyadhar M Paradkar, Haengsoon Park, Laura R Rokosz, Tara M Stauffer, Timothy J Guzi.   

Abstract

Properly substituted pyrazolo[1,5-a]pyrimidines are potent and selective CDK2 inhibitors. Compound 15j is orally available and showed efficacy in a mouse A2780 xenograft model.

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Year:  2007        PMID： 17904841     DOI： 10.1016/j.bmcl.2007.09.017

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


  7 in total

1.  Synthesis and SAR studies of novel 6,7,8-substituted 4-substituted benzyloxyquinolin-2(1H)-one derivatives for anticancer activity.

Authors:  Yi-Fong Chen; Yi-Chien Lin; Susan L Morris-Natschke; Chen-Fang Wei; Ting-Chen Shen; Hui-Yi Lin; Mei-Hua Hsu; Li-Chen Chou; Yu Zhao; Sheng-Chu Kuo; Kuo-Hsiung Lee; Li-Jiau Huang
Journal:  Br J Pharmacol       Date:  2015-01-13       Impact factor: 8.739

2.  Discovery of Dinaciclib (SCH 727965): A Potent and Selective Inhibitor of Cyclin-Dependent Kinases.

Authors:  Kamil Paruch; Michael P Dwyer; Carmen Alvarez; Courtney Brown; Tin-Yau Chan; Ronald J Doll; Kerry Keertikar; Chad Knutson; Brian McKittrick; Jocelyn Rivera; Randall Rossman; Greg Tucker; Thierry Fischmann; Alan Hruza; Vincent Madison; Amin A Nomeir; Yaolin Wang; Paul Kirschmeier; Emma Lees; David Parry; Nicole Sgambellone; Wolfgang Seghezzi; Lesley Schultz; Frances Shanahan; Derek Wiswell; Xiaoying Xu; Quiao Zhou; Ray A James; Vidyadhar M Paradkar; Haengsoon Park; Laura R Rokosz; Tara M Stauffer; Timothy J Guzi
Journal:  ACS Med Chem Lett       Date:  2010-05-17       Impact factor: 4.345

3.  Efficient microwave-assisted Suzuki-Miyaura cross-coupling reaction of 3-bromo pyrazolo[1,5-a]pyrimidin-5(4H)-one: towards a new access to 3,5-diarylated 7-(trifluoromethyl)pyrazolo[1,5-a]pyrimidine derivatives.

Authors:  Badr Jismy; Gérald Guillaumet; Mohamed Akssira; Abdellatif Tikad; Mohamed Abarbri
Journal:  RSC Adv       Date:  2021-01-04       Impact factor: 4.036

4.  Discovery of GSK3β Inhibitors through In Silico Prediction-and-Experiment Cycling Strategy, and Biological Evaluation.

Authors:  Yuno Lee; Sae-Bom Yoon; Hyowon Hong; Hyun Young Kim; Daeyoung Jung; Byoung-San Moon; Woo-Kyu Park; Sunkyung Lee; Hyukjin Kwon; Jihyeong Park; Heeyeong Cho
Journal:  Molecules       Date:  2022-06-14       Impact factor: 4.927

5.  Rationalizing tight ligand binding through cooperative interaction networks.

Authors:  Bernd Kuhn; Julian E Fuchs; Michael Reutlinger; Martin Stahl; Neil R Taylor
Journal:  J Chem Inf Model       Date:  2011-12-09       Impact factor: 4.956

6.  Identification of small molecule modulators of HIV-1 Tat and Rev protein accumulation.

Authors:  Ahalya Balachandran; Raymond Wong; Peter Stoilov; Sandy Pan; Benjamin Blencowe; Peter Cheung; P Richard Harrigan; Alan Cochrane
Journal:  Retrovirology       Date:  2017-01-26       Impact factor: 4.602

7.  Efficient Access to 3,5-Disubstituted 7-(Trifluoromethyl)pyrazolo[1,5-a]pyrimidines Involving SNAr and Suzuki Cross-Coupling Reactions.

Authors:  Badr Jismy; Abdellatif Tikad; Mohamed Akssira; Gérald Guillaumet; Mohamed Abarbri
Journal:  Molecules       Date:  2020-04-28       Impact factor: 4.411
  7 in total

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