Literature DB >> 18835709

Synthesis and evaluation of pyrazolo[1,5-b]pyridazines as selective cyclin dependent kinase inhibitors.

Kirk L Stevens1, Michael J Reno, Jennifer B Alberti, Daniel J Price, Laurie S Kane-Carson, Victoria B Knick, Lisa M Shewchuk, Anne M Hassell, James M Veal, Stephen T Davis, Robert J Griffin, Michael R Peel.   

Abstract

A novel series of pyrazolo[1,5-b]pyridazines have been synthesized and identified as cyclin dependant kinase inhibitors potentially useful for the treatment of solid tumors. Modification of the hinge-binding amine or the C(2)- and C(6)-substitutions on the pyrazolopyridazine core provided potent inhibitors of CDK4 and demonstrated enzyme selectivity against VEGFR-2 and GSK3beta.

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Year:  2008        PMID： 18835709     DOI： 10.1016/j.bmcl.2008.09.069

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


  10 in total

1.  Chemical interrogation of the malaria kinome.

Authors:  Emily R Derbyshire; Vanessa Zuzarte-Luís; Andreia D Magalhães; Nobutaka Kato; Paul C Sanschagrin; Jinhua Wang; Wenjun Zhou; Chandrasekhar V Miduturu; Ralph Mazitschek; Piotr Sliz; Maria M Mota; Nathanael S Gray; Jon Clardy
Journal:  Chembiochem       Date:  2014-08-08       Impact factor: 3.164

2.  GW779439X and Its Pyrazolopyridazine Derivatives Inhibit the Serine/Threonine Kinase Stk1 and Act As Antibiotic Adjuvants against β-Lactam-Resistant Staphylococcus aureus.

Authors:  Adam J Schaenzer; Nathan Wlodarchak; David H Drewry; William J Zuercher; Warren E Rose; Carla A Ferrer; John-Demian Sauer; Rob Striker
Journal:  ACS Infect Dis       Date:  2018-08-15       Impact factor: 5.084

3.  Efficient soluble expression of active recombinant human cyclin A2 mediated by E. coli molecular chaperones.

Authors:  Asterios I Grigoroudis; Campbell McInnes; Padmavathy Nandha Premnath; George Kontopidis
Journal:  Protein Expr Purif       Date:  2015-05-06       Impact factor: 1.650

4.  Antimicrobial evaluation of novel substituted pyrimidinopyrazoles and pyrimidinotriazoles.

Authors:  H S Basavaraja; J E Nagamani; M M J Vijay Kumar; Basavaraj Padmashali
Journal:  J Adv Pharm Technol Res       Date:  2010-04

5.  Evaluation of the published kinase inhibitor set to identify multiple inhibitors of bacterial ATP-dependent mur ligases.

Authors:  Martina Hrast; Kaja Rožman; Iza Ogris; Veronika Škedelj; Delphine Patin; Matej Sova; Hélène Barreteau; Stanislav Gobec; Simona Golič Grdadolnik; Anamarija Zega
Journal:  J Enzyme Inhib Med Chem       Date:  2019-12       Impact factor: 5.051

6.  Engineering Selectivity for Reduced Toxicity of Bacterial Kinase Inhibitors Using Structure-Guided Medicinal Chemistry.

Authors:  Nathan Wlodarchak; John B Feltenberger; Zhengqing Ye; Jeffrey Beczkiewicz; Rebecca Procknow; Gang Yan; Troy M King; Jennifer E Golden; Rob Striker
Journal:  ACS Med Chem Lett       Date:  2021-01-13       Impact factor: 4.345

7.  Profile of the GSK published protein kinase inhibitor set across ATP-dependent and-independent luciferases: implications for reporter-gene assays.

Authors:  Patricia Dranchak; Ryan MacArthur; Rajarshi Guha; William J Zuercher; David H Drewry; Douglas S Auld; James Inglese
Journal:  PLoS One       Date:  2013-03-07       Impact factor: 3.240

8.  Using a Genetically Encoded Sensor to Identify Inhibitors of Toxoplasma gondii Ca2+ Signaling.

Authors:  Saima M Sidik; Miryam A Hortua Triana; Aditya S Paul; Majida El Bakkouri; Caroline G Hackett; Fanny Tran; Nicholas J Westwood; Raymond Hui; William J Zuercher; Manoj T Duraisingh; Silvia N J Moreno; Sebastian Lourido
Journal:  J Biol Chem       Date:  2016-03-01       Impact factor: 5.157

9.  A first generation inhibitor of human Greatwall kinase, enabled by structural and functional characterisation of a minimal kinase domain construct.

Authors:  Cory A Ocasio; Mohan B Rajasekaran; Sarah Walker; Darren Le Grand; John Spencer; Frances M G Pearl; Simon E Ward; Velibor Savic; Laurence H Pearl; Helfrid Hochegger; Antony W Oliver
Journal:  Oncotarget       Date:  2016-11-01

10.  Crystal Structure and Inhibitor Identifications Reveal Targeting Opportunity for the Atypical MAPK Kinase ERK3.

Authors:  Martin Schröder; Panagis Filippakopoulos; Martin P Schwalm; Carla A Ferrer; David H Drewry; Stefan Knapp; Apirat Chaikuad
Journal:  Int J Mol Sci       Date:  2020-10-26       Impact factor: 5.923
  10 in total

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