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Antiproliferative activity of the Michael adducts of aroylacrylic acids and cyclic amines

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2014
Authors
Juranić, Ivan
Tošić, Ana V.
Kolundžija, Branka
Drakulić, Branko
Article (Published version)
,
Springer
Metadata
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Abstract
Antiproliferative activity of twenty one Michael adducts of aroylacrylic acids and cyclic amines ( N -Me-piperazine, imidazole, 2-Me-imidazole, and indole) was tested toward five human tumor cell lines (HeLa, LS174, K562, FemX, MDA-MB-361) in vitro. Compounds exerted antiproliferative activity in the high to the single-digit micromolar concentrations, causing increase of the cell population fraction in S phase and apoptosis. N -Me-piperazine and imidazole derivatives of aroylacrylic acids substituted with bulky alkyl substituents (2,4-di- i -Pr-Ph-, 2,4,6-tri-Et-Ph-, or β -tetrahydronaphthyl-) showed the best potency, while indole adducts were proved as the inferior antiproliferative agents. Few compounds showed significant selectivity, tumor versus healthy cells, with selectivity index ∼60 for the most selective congener. An unbiased in silico distinction between more and less potent compounds was obtained from 3D QSAR models derived by alignment-independent GRIND-2 descripto...rs.

Keywords:
Antiproliferative activity / Selectivity / Michael adducts / Aroylacrylic acids / 3D QSAR
Source:
Molecular Diversity, 2014, 18, 3, 577-592
Publisher:
  • Springer
Projects:
  • Rational design and synthesis of biologically active and coordination compounds and functional materials, relevant for (bio)nanotechnology (RS-172035)

DOI: 10.1007/s11030-014-9528-4

ISSN: 1381-1991

PubMed: 24874228

WoS: 000338641700009

Scopus: 2-s2.0-84903818978
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URI
http://cer.ihtm.bg.ac.rs/handle/123456789/2670
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