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Phenylpropiophenone derivatives as potential anticancer agents: synthesis, biological evaluation and quantitative structure-activity relationship study.

Abstract：

:Series of twelve chalcone and propafenone derivatives has been synthesized and evaluated for anticancer activities against HeLa, Fem-X, PC-3, MCF-7, LS174 and K562 cell lines. The 2D-QSAR and 3D-QSAR studies were performed for all compounds with cytotoxic activities against each cancer cell line. Partial least squares (PLS) regression has been applied for selection of the most relevant molecular descriptors and QSAR models building. Predictive potentials of the created 2D-QSAR and 3D-QSAR models for each cell line were compared, by use of leave-one-out cross-validation and external validation, and optimal QSAR models for each cancer cell line were selected. The QSAR studies have selected the most significant molecular descriptors and pharmacophores of the chalcone and propafenone derivatives and proposed structures of novel chalcone and propafenone derivatives with enhanced anticancer activity on the HeLa, Fem-X, PC-3, MCF-7, LS174 and K562 cells.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Ivković BM,Nikolic K,Ilić BB,Žižak ŽS,Novaković RB,Čudina OA,Vladimirov SM

doi

10.1016/j.ejmech.2013.02.013

subject

Has Abstract

pub_date

2013-05-01 00:00:00

pages

239-55

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(13)00099-8

journal_volume

63

pub_type

杂志文章

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