Literature DB >> 15713378

Benzodipyrazoles: a new class of potent CDK2 inhibitors.

Roberto D'Alessio1, Alberto Bargiotti, Suzanne Metz, M Gabriella Brasca, Alexander Cameron, Antonella Ermoli, Aurelio Marsiglio, Paolo Polucci, Fulvia Roletto, Marcellino Tibolla, Michael L Vazquez, Anna Vulpetti, Paolo Pevarello.   

Abstract

The synthesis and the preliminary expansion of this new class of CDK2 inhibitors are presented. The synthesis was accomplished using a solution-phase protocol amenable to rapid parallel expansion and suitable to be scaled-up in view of possible lead development. Following a medicinal chemistry program aimed at improving cell permeability and selectivity, a series of compounds with nanomolar activity in the biochemical assay and able to efficiently inhibit tumor cell proliferation has been obtained.

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Year:  2005        PMID: 15713378     DOI: 10.1016/j.bmcl.2005.01.023

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


  2 in total

1.  6-Methoxyflavone induces S-phase arrest through the CCNA2/CDK2/p21CIP1 signaling pathway in HeLa cells.

Authors:  Chaihong Zhang; Yuchong Quan; Lijuan Yang; Yingying Bai; Yongxiu Yang
Journal:  Bioengineered       Date:  2022-03       Impact factor: 3.269

2.  OOMMPPAA: a tool to aid directed synthesis by the combined analysis of activity and structural data.

Authors:  Anthony R Bradley; Ian D Wall; Darren V S Green; Charlotte M Deane; Brian D Marsden
Journal:  J Chem Inf Model       Date:  2014-10-09       Impact factor: 4.956

  2 in total

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