Literature DB >> 19836248

3,4-Dihydropyrimido(1,2-a)indol-10(2H)-ones as potent non-peptidic inhibitors of caspase-3.

Lisa M Havran1, Dan C Chong, Wayne E Childers, Paul J Dollings, Arlene Dietrich, Boyd L Harrison, Vasilios Marathias, Gregory Tawa, Ann Aulabaugh, Rebecca Cowling, Bhupesh Kapoor, Weixin Xu, Lidia Mosyak, Franklin Moy, Wah-Tung Hum, Andrew Wood, Albert J Robichaud.   

Abstract

Cysteine-dependant aspartyl protease (caspase) activation has been implicated as a part of the signal transduction pathway leading to apoptosis. It has been postulated that caspase-3 inhibition could attenuate cell damage after an ischemic event and thereby providing for a novel neuroprotective treatment for stroke. As part of a program to develop a small molecule inhibitor of caspase-3, a novel series of 3,4-dihydropyrimido(1,2-a)indol-10(2H)-ones (pyrimidoindolones) was identified. The synthesis, biological evaluation and structure-activity relationships of the pyrimidoindolones are described.

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Year:  2009        PMID: 19836248     DOI: 10.1016/j.bmc.2009.09.036

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN: 0968-0896            Impact factor:   3.641


  3 in total

Review 1.  Small Molecule Active Site Directed Tools for Studying Human Caspases.

Authors:  Marcin Poreba; Aleksandra Szalek; Paulina Kasperkiewicz; Wioletta Rut; Guy S Salvesen; Marcin Drag
Journal:  Chem Rev       Date:  2015-11-09       Impact factor: 60.622

2.  Synthesis and evaluation of isatin analogs as caspase-3 inhibitors: introduction of a hydrophilic group increases potency in a whole cell assay.

Authors:  Wenhua Chu; Justin Rothfuss; Dong Zhou; Robert H Mach
Journal:  Bioorg Med Chem Lett       Date:  2011-04-15       Impact factor: 2.823

3.  Chiral aminophosphines as catalysts for enantioselective double-Michael indoline syntheses.

Authors:  San N Khong; Ohyun Kwon
Journal:  Molecules       Date:  2012-05-11       Impact factor: 4.411

  3 in total

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