Literature DB >> 15686876

Structure-guided design of pyrazolo[1,5-a]pyrimidines as inhibitors of human cyclin-dependent kinase 2.

Douglas S Williamson1, Martin J Parratt, Justin F Bower, Jonathan D Moore, Christine M Richardson, Pawel Dokurno, Andrew D Cansfield, Geraint L Francis, Richard J Hebdon, Rob Howes, Philip S Jackson, Andrea M Lockie, James B Murray, Claire L Nunns, Jenifer Powles, Alan Robertson, Allan E Surgenor, Christopher J Torrance.   

Abstract

The protein structure guided design of a series of pyrazolo[1,5-a]pyrimidines with high potency for human cyclin-dependent kinase 2 (CDK2) is described. Some examples were shown to inhibit the growth of human colon tumour cells, were equipotent for CDK1 and were selective against GSK-3beta and other kinases.

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Year:  2005        PMID： 15686876     DOI： 10.1016/j.bmcl.2004.12.073

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


  6 in total

1.  Potent and Selective Inhibitors of CK2 Kinase Identified through Structure-Guided Hybridization.

Authors:  James E Dowling; Claudio Chuaqui; Timothy W Pontz; Paul D Lyne; Nicholas A Larsen; Michael H Block; Huawei Chen; Nancy Su; Allan Wu; Daniel Russell; Hannah Pollard; John W Lee; Bo Peng; Kumar Thakur; Qing Ye; Tao Zhang; Patrick Brassil; Vicki Racicot; Larry Bao; Christopher R Denz; Emma Cooke
Journal:  ACS Med Chem Lett       Date:  2012-01-24       Impact factor: 4.345

2.  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

3.  The development of a selective cyclin-dependent kinase inhibitor that shows antitumor activity.

Authors:  Simak Ali; Dean A Heathcote; Sebastian H B Kroll; Ashutosh S Jogalekar; Bodo Scheiper; Hetal Patel; Jan Brackow; Alekasandra Siwicka; Matthew J Fuchter; Manikandan Periyasamy; Robert S Tolhurst; Seshu K Kanneganti; James P Snyder; Dennis C Liotta; Eric O Aboagye; Anthony G M Barrett; R Charles Coombes
Journal:  Cancer Res       Date:  2009-07-28       Impact factor: 12.701

4.  Crystal structure of human cyclin-dependent kinase-2 complex with MK2 inhibitor TEI-I01800: insight into the selectivity.

Authors:  Aiko Fujino; Kei Fukushima; Takaharu Kubota; Tomomi Kosugi; Midori Takimoto-Kamimura
Journal:  J Synchrotron Radiat       Date:  2013-09-26       Impact factor: 2.616

5.  Synthesis, Structural Elucidation, and In Vitro Antitumor Activities of Some Pyrazolopyrimidines and Schiff Bases Derived from 5-Amino-3-(arylamino)-1H-pyrazole-4-carboxamides.

Authors:  Taghrid S Hafez; Souad A Osman; Hisham Abdallah A Yosef; Amira S Abd El-All; Ashraf S Hassan; Abdallah A El-Sawy; Mohamed M Abdallah; Mahmoud Youns
Journal:  Sci Pharm       Date:  2013-01-03

6.  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
  6 in total

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