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Arch Pharm (Weinheim). 2011 May;344(5):333-9. doi: 10.1002/ardp.201000194. Epub 2011 Feb 14.

The design and cytotoxic evaluation of some 1-aryl-3-isopropylamino-1-propanone hydrochlorides towards human Huh-7 hepatoma cells.

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1
Department of Chemistry, Faculty of Sciences, Ataturk University, Erzurum, Turkey. ebru25@atauni.edu.tr

Abstract

A series of 1-aryl-3-isopropylamino-1-propanone hydrochlorides 1 and a related heterocyclic analog 2 as candidate antineoplastic agents were prepared and the rationale for designing these compounds is presented. A specific objective in this study is the discovery of novel compounds possessing growth-inhibiting properties of hepatoma cells. The compounds in series 1 and 2 were prepared and their structures established unequivocally. X-ray crystallography of two representative compounds 1d and 1g were achieved. Over half of the compounds are more potent than 5-fluorouracil which is an established drug used in treating liver cancers. QSAR evaluations and molecular modeling studies were undertaken with a view to detecting some physicochemical parameters which govern cytotoxic potencies. A number of guidelines for amplification of the project have been formulated.

PMID:
21319206
PMCID:
PMC3319740
DOI:
10.1002/ardp.201000194
[Indexed for MEDLINE]
Free PMC Article
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