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The Design and Cytotoxic Evaluation of Some 1‐Aryl‐3‐isopropylamino‐1‐propanone Hydrochlorides towards Human Huh‐7 Hepatoma Cells
Author(s) -
Mete Ebru,
Gul H. Inci,
CetinAtalay Rengul,
Das Umashankar,
Sahin Ertan,
Gul Mustafa,
Kazaz Cavit,
Dimmock Jonathan R.
Publication year - 2011
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.201000194
Subject(s) - chemistry , aryl , cytotoxic t cell , stereochemistry , quantitative structure–activity relationship , combinatorial chemistry , tumor cells , cytotoxicity , drug , anticancer drug , pharmacology , biochemistry , in vitro , cancer research , organic chemistry , biology , alkyl
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.