Literature DB >> 24091081

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

Michael P Dwyer1, Kartik Keertikar, Kamil Paruch, Carmen Alvarez, Marc Labroli, Cory Poker, Thierry O Fischmann, Rosemary Mayer-Ezell, Richard Bond, Yan Wang, Rita Azevedo, Timothy J Guzi.   

Abstract

The synthesis and hit-to-lead SAR development from a pyrazolo[1,5-a]pyrimidine-derived hit 5 to the identification of a series of potent, pan-Pim inhibitors such as 11j are described.
Copyright © 2013 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  Pan–Pim kinase; pyrazolo[1,5-a]pyrimidine

Mesh：

Substances：

Year:  2013        PMID： 24091081     DOI： 10.1016/j.bmcl.2013.08.110

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


  6 in total

1.  Synthesis and Biological Evaluation of Pyrazolo[1,5-a]pyrimidine Compounds as Potent and Selective Pim-1 Inhibitors.

Authors:  Yong Xu; Benjamin G Brenning; Steven G Kultgen; Jason M Foulks; Adrianne Clifford; Shuping Lai; Ashley Chan; Shannon Merx; Michael V McCullar; Steven B Kanner; Koc-Kan Ho
Journal:  ACS Med Chem Lett       Date:  2014-10-22       Impact factor: 4.345

2.  Characterization of HJ-PI01 as a novel Pim-2 inhibitor that induces apoptosis and autophagic cell death in triple-negative human breast cancer.

Authors:  Yu-Qian Zhao; Yi-Qiong Yin; Jie Liu; Gui-Hua Wang; Jian Huang; Ling-Juan Zhu; Jin-Hui Wang
Journal:  Acta Pharmacol Sin       Date:  2016-07-11       Impact factor: 6.150

3.  Computational prediction and experimental validation of a novel synthesized pan-PIM inhibitor PI003 and its apoptosis-inducing mechanisms in cervical cancer.

Authors:  Zhongyu Liu; Weihua He; Jianglin Gao; Junhua Luo; Xian Huang; Chunfang Gao
Journal:  Oncotarget       Date:  2015-04-10

4.  Chk1 inhibition significantly potentiates activity of nucleoside analogs in TP53-mutated B-lymphoid cells.

Authors:  Jana Zemanova; Ondrej Hylse; Jana Collakova; Pavel Vesely; Alexandra Oltova; Marek Borsky; Kristina Zaprazna; Marie Kasparkova; Pavlina Janovska; Jan Verner; Jiri Kohoutek; Marta Dzimkova; Vitezslav Bryja; Zuzana Jaskova; Yvona Brychtova; Kamil Paruch; Martin Trbusek
Journal:  Oncotarget       Date:  2016-09-20

5.  Distinct cellular responses to replication stress leading to apoptosis or senescence.

Authors:  Emilie Lukášová; Martina Řezáčová; Alena Bačíková; Ludmila Šebejová; Jiřina Vávrová; Stanislav Kozubek
Journal:  FEBS Open Bio       Date:  2019-04-13       Impact factor: 2.693

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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