Literature DB >> 23870430

2-Amino-[1,2,4]triazolo[1,5-a]pyridines as JAK2 inhibitors.

Michael Siu1, Richard Pastor, Wendy Liu, Kathy Barrett, Megan Berry, Wade S Blair, Christine Chang, Jacob Z Chen, Charles Eigenbrot, Nico Ghilardi, Paul Gibbons, Haiying He, Christopher A Hurley, Jane R Kenny, S Cyrus Khojasteh, Hoa Le, Leslie Lee, Joseph P Lyssikatos, Steve Magnuson, Rebecca Pulk, Vickie Tsui, Mark Ultsch, Yisong Xiao, Bing-yan Zhu, Deepak Sampath.   

Abstract

The advancement of a series of ligand efficient 2-amino-[1,2,4]triazolo[1,5-a]pyridines, initially identified from high-throughput screening, to a JAK2 inhibitor with pharmacodynamic activity in a mouse xenograft model is disclosed.
Copyright © 2013 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  JAK2; Janus kinase; Triazolopyridine

Mesh：

Substances：

Year:  2013        PMID： 23870430     DOI： 10.1016/j.bmcl.2013.06.008

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


  7 in total

1.  AlphaSpace 2.0: Representing Concave Biomolecular Surfaces Using β-Clusters.

Authors:  Joseph Katigbak; Haotian Li; David Rooklin; Yingkai Zhang
Journal:  J Chem Inf Model       Date:  2020-02-11       Impact factor: 4.956

2.  A computationally affordable approach for accurate prediction of the binding affinity of JAK2 inhibitors.

Authors:  Nguyen Thi Mai; Ngo Thi Lan; Thien Y Vu; Nguyen Thanh Tung; Huong Thi Thu Phung
Journal:  J Mol Model       Date:  2022-05-23       Impact factor: 1.810

Review 3.  Dual-target inhibitors of bromodomain and extra-terminal proteins in cancer: A review from medicinal chemistry perspectives.

Authors:  Lu Feng; Guan Wang; Yi Chen; Gu He; Bo Liu; Jie Liu; Cheng-Ming Chiang; Liang Ouyang
Journal:  Med Res Rev       Date:  2021-10-11       Impact factor: 12.944

4.  Effect of 6,7-dimethoxy-2,2-dimethyl-2H-chromene (agerarin) on the recovery of filaggrin expression through targeting of Janus kinases in the inflammatory skin.

Authors:  Sung Shin Ahn; Young Han Lee; Hyunjin Yeo; Youngshim Lee; Do Sik Min; Yoongho Lim; Soon Young Shin
Journal:  J Food Drug Anal       Date:  2020-09-15       Impact factor: 6.157

5.  Resolving TYK2 locus genotype-to-phenotype differences in autoimmunity.

Authors:  Calliope A Dendrou; Adrian Cortes; Lydia Shipman; Hayley G Evans; Kathrine E Attfield; Luke Jostins; Thomas Barber; Gurman Kaur; Subita Balaram Kuttikkatte; Oliver A Leach; Christiane Desel; Soren L Faergeman; Jane Cheeseman; Matt J Neville; Stephen Sawcer; Alastair Compston; Adam R Johnson; Christine Everett; John I Bell; Fredrik Karpe; Mark Ultsch; Charles Eigenbrot; Gil McVean; Lars Fugger
Journal:  Sci Transl Med       Date:  2016-11-02       Impact factor: 17.956

6.  KI-catalyzed oxidative cyclization of α-keto acids and 2-hydrazinopyridines: efficient one-pot synthesis of 1,2,4-triazolo[4,3-a]pyridines.

Authors:  De-Suo Yang; Juan Wang; Peng Gao; Zi-Jing Bai; Dong-Zhu Duan; Ming-Jin Fan
Journal:  RSC Adv       Date:  2018-09-21       Impact factor: 3.361

7.  Dual kinase-bromodomain inhibitors for rationally designed polypharmacology.

Authors:  Pietro Ciceri; Susanne Müller; Alison O'Mahony; Oleg Fedorov; Panagis Filippakopoulos; Jeremy P Hunt; Elisabeth A Lasater; Gabriel Pallares; Sarah Picaud; Christopher Wells; Sarah Martin; Lisa M Wodicka; Neil P Shah; Daniel K Treiber; Stefan Knapp
Journal:  Nat Chem Biol       Date:  2014-03-02       Impact factor: 15.040
  7 in total

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