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

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

  • Eur J Med Chem. 2011 Mar;46(3):953-60. doi: 10.1016/j.ejmech.2010.12.013.
Feng Shi 1,  An-Xiao Dai,  Shu Zhang,  Xiao-Hong Zhang,  Shu-Jiang Tu
Affiliations

Affiliation

  • 1 College of Chemistry, Chemical Engineering and Materials Science, Soochow University, Suzhou 215000, PR China.
PMID: 21247667 DOI: 10.1016/j.ejmech.2010.12.013
Abstract

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. Nearly all the tested compounds exhibited strong or moderate cytotoxicity to SGC7901 cells with IC(50) values from 5.127 to 0.158 ug/mL.

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