Facile diversity-oriented synthesis of novel dipeptide mimetic compounds containing bioactive molecular skeletons under microwave irradiation.

The diversity-oriented synthesis of dipeptide mimetic compounds embedded with bioactive molecular skeletons have been successfully established via microwave-assisted reactions between various 4-arylidene-2-phenyloxazol-5(4H)-ones and a broad scope of amines including aliphatic, aromatic, and heteroaromatic ones. This synthetic approach has prominent features of short reaction time, high yields, operational simplicity, as well as widespread applications, leading to a facile and straightforward access to structurally diverse dipeptide analogues with potential bioactivities. Moreover, the preliminary evaluation on the cytotoxic activity of this type of dipeptide derivatives has resulted in the finding of five compounds with stronger cytotoxicity than doxorubicin hydrochloride at the concentration of 10 μg/mL.

Efficient microwave-assisted synthesis of novel 3-aminohexahydrocoumarin derivatives and evaluation on their cytotoxicity.

The efficient synthesis of novel 3-aminohexahydrocoumarin derivatives with high diastereoselectivity, wide applicability, short reaction time, high yields as well as operational simplicity was achieved via microwave-assisted reactions of dimedone or cyclohexane-1,3-dione with 4-arylidene-2-phenyloxazol-5(4H)-ones. Moreover, these novel compounds were subject to the test of in vitro cytotoxicity to carcinoma SW1116 and SGC7901 cells. Seven compounds showed stronger cytotoxicity to carcinoma SW1116 cells than doxorubicin hydrochloride at the concentration of 10 ug/mL.