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

► This study has achieved the efficient synthesis of novel 3-aminohexahydrocoumarin derivatives and examined their in vitro cytotoxic activity. This study provides a facile shortcut for the synthesis of 3-aminohexahydrocoumarin derivatives with high diastereoselectivity, wide applicability, short reaction time, high yields as well as operational simplicity. More importantly, bioassay of these novel 3-aminohexahydrocoumarin derivatives resulted in the finding of seven compounds with stronger cytotoxicity to carcinoma SW1116 cells than doxorubicin hydrochloride at the same concentration, which gains some insights into the synthesis or structure modifications of 3-aminohexahydrocoumarin derivatives for the purpose of discovering new anti-cancer drug candidates.