Literature DB >> 21094608

Discovery of pyrazolo[1,5-a]pyrimidine-based CHK1 inhibitors: a template-based approach--part 1.

Michael P Dwyer1, Kamil Paruch, Marc Labroli, Carmen Alvarez, Kerry M Keertikar, Cory Poker, Randall Rossman, Thierry O Fischmann, Jose S Duca, Vincent Madison, David Parry, Nicole Davis, Wolfgang Seghezzi, Derek Wiswell, Timothy J Guzi.   

Abstract

The synthesis and hit-to-lead SAR development of a pyrazolo[1,5-a]pyrimidine hit 4 is described leading to a series of potent, selective CHK1 inhibitors such as compound 17r. In the Letter, the further utility of the pyrazolo[1,5-a]pyrimidine template for the development of potent, selective kinase inhibitors is detailed.
Copyright © 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID： 21094608     DOI： 10.1016/j.bmcl.2010.10.113

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


  11 in total

1.  Small Molecule Amyloid-β Protein Precursor Processing Modulators Lower Amyloid-β Peptide Levels via cKit Signaling.

Authors:  Ci-Di Chen; Ella Zeldich; Christina Khodr; Kaddy Camara; Tze Yu Tung; Emma C Lauder; Patrick Mullen; Taryn J Polanco; Yen-Yu Liu; Dean Zeldich; Weiming Xia; William E Van Nostrand; Lauren E Brown; John A Porco; Carmela R Abraham
Journal:  J Alzheimers Dis       Date:  2019       Impact factor: 4.472

2.  A facile, regioselective synthesis of novel 3-(N-phenylcarboxamide)pyrazolo[1,5-a]pyrimidine analogs in the presence of KHSO4 in aqueous media assisted by ultrasound and their antibacterial activities.

Authors:  Shunan Kaping; Ivee Boiss; Laishram Indira Singha; Philippe Helissey; Jai N Vishwakarma
Journal:  Mol Divers       Date:  2015-10-28       Impact factor: 2.943

3.  Discovery of a Novel Series of CHK1 Kinase Inhibitors with a Distinctive Hinge Binding Mode.

Authors:  Xiaohua Huang; Cliff C Cheng; Thierry O Fischmann; José S Duca; Xianshu Yang; Matthew Richards; Gerald W Shipps
Journal:  ACS Med Chem Lett       Date:  2012-01-20       Impact factor: 4.345

4.  Structural requirements of pyrimidine, thienopyridine and ureido thiophene carboxamide-based inhibitors of the checkpoint kinase 1: QSAR, docking, molecular dynamics analysis.

Authors:  Fangfang Wang; Zhi Ma; Yan Li; Jinan Wang; Yonghua Wang
Journal:  J Mol Model       Date:  2012-01-15       Impact factor: 1.810

5.  A facile environment-friendly one-pot two-step regioselective synthetic strategy for 3,7-diarylpyrazolo[1,5-a]pyrimidines related to zaleplon and 3,6-diarylpyrazolo[1,5-a]pyrimidine-7-amines assisted by KHSO₄ in aqueous media.

Authors:  Asem Satyapati Devi; Shunan Kaping; Jai Narain Vishwakarma
Journal:  Mol Divers       Date:  2015-05-28       Impact factor: 2.943

Review 6.  Structure-based design, discovery and development of checkpoint kinase inhibitors as potential anticancer therapies.

Authors:  Thomas P Matthews; Alan M Jones; Ian Collins
Journal:  Expert Opin Drug Discov       Date:  2013-04-18       Impact factor: 6.098

7.  BRG1 Loss Predisposes Lung Cancers to Replicative Stress and ATR Dependency.

Authors:  Manav Gupta; Carla P Concepcion; Caroline G Fahey; Hasmik Keshishian; Arjun Bhutkar; Christine F Brainson; Francisco J Sanchez-Rivera; Patrizia Pessina; Jonathan Y Kim; Antoine Simoneau; Margherita Paschini; Mary C Beytagh; Caroline R Stanclift; Monica Schenone; D R Mani; Chendi Li; Audris Oh; Fei Li; Hai Hu; Angeliki Karatza; Roderick T Bronson; Alice T Shaw; Aaron N Hata; Kwok-Kin Wong; Lee Zou; Steven A Carr; Tyler Jacks; Carla F Kim
Journal:  Cancer Res       Date:  2020-07-20       Impact factor: 12.701

8.  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

Review 9.  5-Aminopyrazole as precursor in design and synthesis of fused pyrazoloazines.

Authors:  Ranjana Aggarwal; Suresh Kumar
Journal:  Beilstein J Org Chem       Date:  2018-01-25       Impact factor: 2.883

10.  Imidazopyridazines as potent inhibitors of Plasmodium falciparum calcium-dependent protein kinase 1 (PfCDPK1): Preparation and evaluation of pyrazole linked analogues.

Authors:  Jonathan M Large; Simon A Osborne; Ela Smiljanic-Hurley; Keith H Ansell; Hayley M Jones; Debra L Taylor; Barbara Clough; Judith L Green; Anthony A Holder
Journal:  Bioorg Med Chem Lett       Date:  2013-08-11       Impact factor: 2.823
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