Literature DB >> 15974571

1-Acyl-1H-[1,2,4]triazole-3,5-diamine analogues as novel and potent anticancer cyclin-dependent kinase inhibitors: synthesis and evaluation of biological activities.

Ronghui Lin1, Peter J Connolly, Shenlin Huang, Steven K Wetter, Yanhua Lu, William V Murray, Stuart L Emanuel, Robert H Gruninger, Angel R Fuentes-Pesquera, Catherine A Rugg, Steven A Middleton, Linda K Jolliffe.   

Abstract

A series of 1-acyl-1H-[1,2,4]triazole-3,5-diamine analogues were synthesized as cyclin-dependent kinase (CDK) inhibitors. These compounds showed potent and selective CDK1 and CDK2 inhibitory activities and inhibited in vitro cellular proliferation in various human tumor cells. Representative compound 3b demonstrated in vivo efficacy in a human melanoma A375 xenograft model in nude mice.

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Year:  2005        PMID: 15974571     DOI: 10.1021/jm050267e

Source DB:  PubMed          Journal:  J Med Chem        ISSN: 0022-2623            Impact factor:   7.446


  21 in total

1.  Selective Janus Kinase 2 (JAK2) Pseudokinase Ligands with a Diaminotriazole Core.

Authors:  Maria-Elena Liosi; Stefan G Krimmer; Ana S Newton; Thomas K Dawson; David E Puleo; Kara J Cutrona; Yoshihisa Suzuki; Joseph Schlessinger; William L Jorgensen
Journal:  J Med Chem       Date:  2020-05-08       Impact factor: 7.446

Review 2.  Cell cycle kinases as therapeutic targets for cancer.

Authors:  Silvia Lapenna; Antonio Giordano
Journal:  Nat Rev Drug Discov       Date:  2009-07       Impact factor: 84.694

3.  JAK2 JH2 Fluorescence Polarization Assay and Crystal Structures for Complexes with Three Small Molecules.

Authors:  Ana S Newton; Luca Deiana; David E Puleo; José A Cisneros; Kara J Cutrona; Joseph Schlessinger; William L Jorgensen
Journal:  ACS Med Chem Lett       Date:  2017-05-17       Impact factor: 4.345

4.  Identification and Characterization of JAK2 Pseudokinase Domain Small Molecule Binders.

Authors:  David E Puleo; Kaury Kucera; Henrik M Hammarén; Daniela Ungureanu; Ana S Newton; Olli Silvennoinen; William L Jorgensen; Joseph Schlessinger
Journal:  ACS Med Chem Lett       Date:  2017-05-17       Impact factor: 4.345

5.  A Precise Cdk Activity Threshold Determines Passage through the Restriction Point.

Authors:  Clayton Schwarz; Amy Johnson; Mardo Kõivomägi; Evgeny Zatulovskiy; Carolyn J Kravitz; Andreas Doncic; Jan M Skotheim
Journal:  Mol Cell       Date:  2018-01-18       Impact factor: 17.970

6.  In silico Screening and Evaluation of Plasmodium falciparum Protein Kinase 5 (PK5) Inhibitors.

Authors:  Amber L Eubanks; Marisha M Perkins; Kayla Sylvester; Jack G Ganley; Dora Posfai; Paul C Sanschargrin; Jiyong Hong; Piotr Sliz; Emily R Derbyshire
Journal:  ChemMedChem       Date:  2018-11-08       Impact factor: 3.466

7.  Analyzing Resistance to Design Selective Chemical Inhibitors for AAA Proteins.

Authors:  Rudolf Pisa; Tommaso Cupido; Jonathan B Steinman; Natalie H Jones; Tarun M Kapoor
Journal:  Cell Chem Biol       Date:  2019-06-27       Impact factor: 8.116

8.  4-n-Butyl-3-(3-methyl-phen-yl)-1H-1,2,4-triazol-5(4H)-one.

Authors:  Tashfeen Akhtar; Shahid Hameed; Muhammad Zia-Ur-Rehman; Tanveer Hussain Bukhari; Islamullah Khan
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2008-07-05

9.  Discovery of Diverse Small-Molecule Inhibitors of Mammalian Sterile20-like Kinase 3 (MST3).

Authors:  Sanne H Olesen; Jin-Yi Zhu; Mathew P Martin; Ernst Schönbrunn
Journal:  ChemMedChem       Date:  2016-05-02       Impact factor: 3.466

10.  Discovery of a first-in-class CDK2 selective degrader for AML differentiation therapy.

Authors:  Liguo Wang; Xuejing Shao; Tianbai Zhong; Yue Wu; Aixiao Xu; Xiuyun Sun; Hongying Gao; Yongbo Liu; Tianlong Lan; Yan Tong; Xue Tao; Wenxin Du; Wei Wang; Yingqian Chen; Ting Li; Xianbin Meng; Haiteng Deng; Bo Yang; Qiaojun He; Meidan Ying; Yu Rao
Journal:  Nat Chem Biol       Date:  2021-03-04       Impact factor: 15.040

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