2,3-dibenzylbutyrolactones and 1,2,3,4-tetrahydro-2-naphthoic acid gamma-lactones: structure and activity relationship in cytotoxic activity.

Dibenzyl-g-butyrolactone and 1,2,3,4-tetrahydro-2-naphthoic acid gamma-lactone (TNL) derivatives were synthesized and evaluated for cytotoxic activity against some cancer cell lines. It was found that TNL derivatives with a shorter distance between C-4 in ring A and C'-2 in ring C were more cytotoxic, while dibenzyl-gamma-butyrolactones with a longer one were nearly inactive. In TNL series, presence of 3,4-dioxy group in ring A and 2-methoxy group in ring C was essential for the enhancement of the activity.