Literature DB >> 30343954

Synthesis of aminopyrazole analogs and their evaluation as CDK inhibitors for cancer therapy.

Sandeep Rana1, Yogesh A Sonawane1, Margaret A Taylor1, Smitha Kizhake1, Muhammad Zahid2, Amarnath Natarajan3.   

Abstract

We synthesized a library of aminopyrazole analogs to systematically explore the hydrophobic pocket adjacent to the hinge region and the solvent exposed region of cyclin dependent kinases. Structure-activity relationship studies identified an optimal substitution for the hydrophobic pocket and analog 24 as a potent and selective CDK2/5 inhibitor.
Copyright © 2018 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  Aminopyrazole; Cyclin dependent kinase 2; Cyclin dependent kinase 5; Growth inhibition

Mesh：

Substances：

Year:  2018        PMID： 30343954      PMCID： PMC6295223          DOI： 10.1016/j.bmcl.2018.10.020

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


  34 in total

1.  Design and synthesis of 1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazoles and pyrazolo[3,4-b]pyridines for Aurora-A kinase inhibitors.

Authors:  Jianyou Shi; Guobin Xu; Wei Zhu; Haoyu Ye; Shengyong Yang; Youfu Luo; Jing Han; Jincheng Yang; Rui Li; Yuquan Wei; Lijuan Chen
Journal:  Bioorg Med Chem Lett       Date:  2010-05-10       Impact factor: 2.823

Review 2.  Caspase activity assays.

Authors:  Andrew L Niles; Richard A Moravec; Terry L Riss
Journal:  Methods Mol Biol       Date:  2008

3.  Development of 1-((1,4-trans)-4-Aryloxycyclohexyl)-3-arylurea Activators of Heme-Regulated Inhibitor as Selective Activators of the Eukaryotic Initiation Factor 2 Alpha (eIF2α) Phosphorylation Arm of the Integrated Endoplasmic Reticulum Stress Response.

Authors:  Revital Yefidoff-Freedman; Jing Fan; Lu Yan; Qingwen Zhang; Guillermo Rodrigo Reis Dos Santos; Sandeep Rana; Jacob I Contreras; Rupam Sahoo; Debin Wan; Jun Young; Karina Luiza Dias Teixeira; Christophe Morisseau; Jose Halperin; Bruce Hammock; Amarnath Natarajan; Peimin Wang; Michael Chorev; Bertal H Aktas
Journal:  J Med Chem       Date:  2017-06-19       Impact factor: 7.446

Review 4.  The history and future of targeting cyclin-dependent kinases in cancer therapy.

Authors:  Uzma Asghar; Agnieszka K Witkiewicz; Nicholas C Turner; Erik S Knudsen
Journal:  Nat Rev Drug Discov       Date:  2015-02       Impact factor: 84.694

5.  Inhibiting the cyclin-dependent kinase CDK5 blocks pancreatic cancer formation and progression through the suppression of Ras-Ral signaling.

Authors:  Georg Feldmann; Anjali Mishra; Seung-Mo Hong; Savita Bisht; Christopher J Strock; Douglas W Ball; Michael Goggins; Anirban Maitra; Barry D Nelkin
Journal:  Cancer Res       Date:  2010-05-18       Impact factor: 12.701

6.  Discovery of a Highly Selective, Brain-Penetrant Aminopyrazole LRRK2 Inhibitor.

Authors:  Bryan K Chan; Anthony A Estrada; Huifen Chen; John Atherall; Charles Baker-Glenn; Alan Beresford; Daniel J Burdick; Mark Chambers; Sara L Dominguez; Jason Drummond; Andrew Gill; Tracy Kleinheinz; Claire E Le Pichon; Andrew D Medhurst; Xingrong Liu; John G Moffat; Kevin Nash; Kimberly Scearce-Levie; Zejuan Sheng; Daniel G Shore; Hervé Van de Poël; Shuo Zhang; Haitao Zhu; Zachary K Sweeney
Journal:  ACS Med Chem Lett       Date:  2012-11-23       Impact factor: 4.345

Review 7.  The Emerging Role of Cdk5 in Cancer.

Authors:  Karine Pozo; James A Bibb
Journal:  Trends Cancer       Date:  2016-10

8.  Design and synthesis of highly potent and isoform selective JNK3 inhibitors: SAR studies on aminopyrazole derivatives.

Authors:  Ke Zheng; Sarah Iqbal; Pamela Hernandez; HaJeung Park; Philip V LoGrasso; Yangbo Feng
Journal:  J Med Chem       Date:  2014-11-21       Impact factor: 7.446

9.  A Phase I study of cyclin-dependent kinase inhibitor, AT7519, in patients with advanced cancer: NCIC Clinical Trials Group IND 177.

Authors:  E X Chen; S Hotte; H Hirte; L L Siu; J Lyons; M Squires; S Lovell; S Turner; L McIntosh; L Seymour
Journal:  Br J Cancer       Date:  2014-11-13       Impact factor: 7.640

10.  Characterization of CDK(5) inhibitor, 20-223 (aka CP668863) for colorectal cancer therapy.

Authors:  Caroline M Robb; Smit Kour; Jacob I Contreras; Ekta Agarwal; Carter J Barger; Sandeep Rana; Yogesh Sonawane; Beth K Neilsen; Margaret Taylor; Smitha Kizhake; Rhishikesh N Thakare; Sanjib Chowdhury; Jing Wang; Jennifer D Black; Michael A Hollingsworth; Michael G Brattain; Amarnath Natarajan
Journal:  Oncotarget       Date:  2017-12-28
View more
  9 in total

1.  Selective degradation of CDK6 by a palbociclib based PROTAC.

Authors:  Sandeep Rana; Mourad Bendjennat; Smit Kour; Hannah M King; Smitha Kizhake; Muhammad Zahid; Amarnath Natarajan
Journal:  Bioorg Med Chem Lett       Date:  2019-03-26       Impact factor: 2.823

Review 2.  Evaluation of Substituted Pyrazole-Based Kinase Inhibitors in One Decade (2011-2020): Current Status and Future Prospects.

Authors:  Mohammed I El-Gamal; Seyed-Omar Zaraei; Moustafa M Madkour; Hanan S Anbar
Journal:  Molecules       Date:  2022-01-05       Impact factor: 4.411

3.  Systemic Administration of a Brain Permeable Cdk5 Inhibitor Alters Neurobehavior.

Authors:  Alan Umfress; Sarbjit Singh; Kevin J Ryan; Ayanabha Chakraborti; Florian Plattner; Yogesh Sonawane; Jayapal Reddy Mallareddy; Edward P Acosta; Amarnath Natarajan; James A Bibb
Journal:  Front Pharmacol       Date:  2022-05-12       Impact factor: 5.988

4.  Spirocyclic dimer SpiD7 activates the unfolded protein response to selectively inhibit growth and induce apoptosis of cancer cells.

Authors:  Smit Kour; Sandeep Rana; Sydney P Kubica; Smitha Kizhake; Mudassier Ahmad; Catalina Muñoz-Trujillo; David Klinkebiel; Sarbjit Singh; Jayapal Reddy Mallareddy; Surabhi Chandra; Nicholas T Woods; Adam R Karpf; Amarnath Natarajan
Journal:  J Biol Chem       Date:  2022-04-01       Impact factor: 5.486

5.  Aminopyrazole based CDK9 PROTAC sensitizes pancreatic cancer cells to venetoclax.

Authors:  Hannah M King; Sandeep Rana; Sydney P Kubica; Jayapal Reddy Mallareddy; Smitha Kizhake; Edward L Ezell; Muhammad Zahid; Michael J Naldrett; Sophie Alvarez; Henry C-H Law; Nicholas T Woods; Amarnath Natarajan
Journal:  Bioorg Med Chem Lett       Date:  2021-04-23       Impact factor: 2.940

6.  CDK5 Inhibitor Downregulates Mcl-1 and Sensitizes Pancreatic Cancer Cell Lines to Navitoclax.

Authors:  Smit Kour; Sandeep Rana; Jacob I Contreras; Hannah M King; Caroline M Robb; Yogesh A Sonawane; Mourad Bendjennat; Ayrianne J Crawford; Carter J Barger; Smitha Kizhake; Xu Luo; Michael A Hollingsworth; Amarnath Natarajan
Journal:  Mol Pharmacol       Date:  2019-10       Impact factor: 4.436

7.  Antileishmanial Aminopyrazoles: Studies into Mechanisms and Stability of Experimental Drug Resistance.

Authors:  M Van den Kerkhof; D Mabille; S Hendrickx; P Leprohon; C E Mowbray; S Braillard; M Ouellette; L Maes; G Caljon
Journal:  Antimicrob Agents Chemother       Date:  2020-08-20       Impact factor: 5.191

Review 8.  Inhibitors, PROTACs and Molecular Glues as Diverse Therapeutic Modalities to Target Cyclin-Dependent Kinase.

Authors:  Sandeep Rana; Jayapal Reddy Mallareddy; Sarbjit Singh; Lidia Boghean; Amarnath Natarajan
Journal:  Cancers (Basel)       Date:  2021-11-02       Impact factor: 6.639

9.  Structure activity relationship (SAR) study identifies a quinoxaline urea analog that modulates IKKβ phosphorylation for pancreatic cancer therapy.

Authors:  Satish Sagar; Sarbjit Singh; Jayapal Reddy Mallareddy; Yogesh A Sonawane; John V Napoleon; Sandeep Rana; Jacob I Contreras; Christabelle Rajesh; Edward L Ezell; Smitha Kizhake; Jered C Garrison; Prakash Radhakrishnan; Amarnath Natarajan
Journal:  Eur J Med Chem       Date:  2021-05-30       Impact factor: 7.088
  9 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.