The Design and Cytotoxic Evaluation of Some 1-Aryl-3-isopropylamino-1-propanone Hydrochlorides towards Human Huh-7 Hepatoma Cells

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METE E., GÜL H. İ., Cetin-Atalay R., Das U., ŞAHİN E., GÜL M., ...Daha Fazla

ARCHIV DER PHARMAZIE, cilt.344, sa.5, ss.333-339, 2011 (SCI-Expanded, Scopus)

Özet

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.