Literature DB >> 15745803

Pyrazolo[1,5-a]pyrimidin-7-yl phenyl amides as novel anti-proliferative agents: parallel synthesis for lead optimization of amide region.

Ariamala Gopalsamy1, Hui Yang, John W Ellingboe, Hwei-Ru Tsou, Nan Zhang, Erick Honores, Dennis Powell, Miriam Miranda, John P McGinnis, Sridhar K Rabindran.   

Abstract

A novel series of p21 chemoselective agents containing a pyrazolo[1,5-a]pyrimidin-7-yl phenyl amides were identified by high throughput screening. Optimization of the amide region by parallel synthesis and the iterative design toward understanding structure-activity relationship to improve potency are described. The isopropyl carbamate derivative 34 was identified as a highly chemoselective agent displaying a potency of 51 nM in the p21 deficient cell line.

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Year:  2005        PMID: 15745803     DOI: 10.1016/j.bmcl.2005.01.066

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


  4 in total

1.  Regioselective multi-component synthesis of 1H-pyrazolo[3,4-d]pyrimidine-6(7H)-thiones.

Authors:  Shirin Safaei; Iraj Mohammadpoor-Baltork; Ahmad Reza Khosropour; Majid Moghadam; Shahram Tangestaninejad; Valiollah Mirkhani
Journal:  Mol Divers       Date:  2012-08-29       Impact factor: 2.943

2.  Approaches towards the synthesis of 5-aminopyrazoles.

Authors:  Ranjana Aggarwal; Vinod Kumar; Rajiv Kumar; Shiv P Singh
Journal:  Beilstein J Org Chem       Date:  2011-02-09       Impact factor: 2.883

3.  7-Chloro-5-(chloro-meth-yl)pyrazolo-[1,5-a]pyrimidine-3-carbonitrile.

Authors:  Jingli Xu; Hang Liu; Guixia Li; Chuanmin Qi
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2012-03-24

4.  18F-labeled pyrazolo[1,5-a]pyrimidine derivatives: synthesis from 2,4-dinitrobenzamide and tosylate precursors and comparative biological evaluation for tumor imaging with positron emission tomography.

Authors:  Jingli Xu; Hang Liu; Guixia Li; Yong He; Rui Ding; Xiao Wang; Man Feng; Shuting Zhang; Yurong Chen; Shilei Li; Mingxia Zhao; Yingruo Li; Chuanmin Qi; Yonghong Dang
Journal:  Molecules       Date:  2012-03-27       Impact factor: 4.411

  4 in total

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