2631-57-4Relevant academic research and scientific papers
The design and cytotoxic evaluation of some 1-aryl-3-isopropylamino-1- propanone hydrochlorides towards human Huh-7 hepatoma cells
Mete, Ebru,Gul, H. Inci,Cetin-Atalay, Rengul,Das, Umashankar,Sahin, Ertan,Gul, Mustafa,Kazaz, Cavit,Dimmock, Jonathan R.
experimental part, p. 333 - 339 (2011/11/05)
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. A number of Mannich bases displayed greater potency than the reference drug 5-fluorouracil against human Huh-7 hepatoma cells. In particular, 1i emerged as a lead compound possessing 2.8 fold higher activity than that of the reference drug. Copyright
