Semisynthesis of triptolide analogues: effect of B-ring substituents on cytotoxic activities.

ABSTRACT

A series of B-ring modified analogues of triptolide were synthesized and tested for their cytotoxicity against two human tumor cell lines (U251 and PC-3). From the current investigation, the structure-cytotoxic activity relationships of these analogues suggested that the introduction of hydroxyl, epoxide, halogen or olefinic groups on C5 and/or C6 could still retain the cytotoxicity, albeit a little less potency, and the C7,C8-ß-epoxide group of triptolide was essential to its potent cytotoxic activity.