Literature DB >> 22266039

Hit to lead evaluation of 1,2,3-triazolo[4,5-b]pyridines as PIM kinase inhibitors.

Joaquín Pastor1, Julen Oyarzabal, Gustavo Saluste, Rosa María Alvarez, Virginia Rivero, Francisco Ramos, Elena Cendón, Carmen Blanco-Aparicio, Nuria Ajenjo, Antonio Cebriá, M I Albarrán, David Cebrián, Ana Corrionero, Jesús Fominaya, Guillermo Montoya, Marco Mazzorana.   

Abstract

PIM kinases have become targets of interest due to their association with biochemical mechanisms affecting survival, proliferation and cytokine production. 1,2,3-Triazolo[4,5-b]pyridines were identified as PIM inhibitors applying a scaffold hopping approach. Initial exploration around this scaffold and X-ray crystallographic data are hereby described.
Copyright © 2012 Elsevier Ltd. All rights reserved.

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Year:  2012        PMID: 22266039     DOI: 10.1016/j.bmcl.2011.12.130

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


  5 in total

1.  Identification of novel inhibitors for Pim-1 kinase using pharmacophore modeling based on a novel method for selecting pharmacophore generation subsets.

Authors:  Rand Shahin; Lubna Swellmeen; Omar Shaheen; Nour Aboalhaija; Maha Habash
Journal:  J Comput Aided Mol Des       Date:  2015-12-19       Impact factor: 3.686

2.  Identification of potent Yes1 kinase inhibitors using a library screening approach.

Authors:  Paresma R Patel; Hongmao Sun; Samuel Q Li; Min Shen; Javed Khan; Craig J Thomas; Mindy I Davis
Journal:  Bioorg Med Chem Lett       Date:  2013-05-29       Impact factor: 2.823

3.  Metal-free domino amination-Knoevenagel condensation approach to access new coumarins as potent nanomolar inhibitors of VEGFR-2 and EGFR.

Authors:  Essam M Eliwa; Marcel Frese; Ahmed H Halawa; Maha M Soltan; Larissa V Ponomareva; Jon S Thorson; Khaled A Shaaban; Mohamed Shaaban; Ahmed M El-Agrody; Norbert Sewald
Journal:  Green Chem Lett Rev       Date:  2021-09-24       Impact factor: 6.016

4.  Fragment-hopping-based discovery of a novel chemical series of proto-oncogene PIM-1 kinase inhibitors.

Authors:  Gustavo Saluste; Maria I Albarran; Rosa M Alvarez; Obdulia Rabal; Miguel Angel Ortega; Carmen Blanco; Guido Kurz; Antonio Salgado; Paolo Pevarello; James R Bischoff; Joaquin Pastor; Julen Oyarzabal
Journal:  PLoS One       Date:  2012-10-24       Impact factor: 3.240

5.  Crystal structure of pim1 kinase in complex with a pyrido[4,3-d]pyrimidine derivative suggests a unique binding mode.

Authors:  Sang Jae Lee; Byeong-Gu Han; Jea-Won Cho; Jang-Sik Choi; Jaekyoo Lee; Ho-Juhn Song; Jong Sung Koh; Byung Il Lee
Journal:  PLoS One       Date:  2013-07-31       Impact factor: 3.240

  5 in total

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