Synthesis of mono- and bifunctional .alpha.-methylene lactone systems as potential tumor inhibitors

Abstract

Synthetic mono- and bifunctional .alpha.-methylene lactone derivatives including deoxyvernolepin and dihydrodeoxyvernolepin were tested as inhibitors of the growth tested as inhibitors of the growth of CCRF-CEM human lymphoblastic leukemia cells in culture. The range of ID50 [median inhibitory dose] values for 7 compounds (10-5-10-6 M) was roughly comparable to the doses observed earlier in the CCRF-CEM cell system with synthetic .alpha.-methylene-.gamma.-butyrolactones. Of significance is that dihydrodeoxyvernolepin and deoxyvernolepin were at least an order of magnitude more active than natural vernolepin.