Synthesis and biological evaluation of didemnin photoaffinity analogues

The synthesis of four benzophenone-containing analogues of the antiprolifer ative natural product didemnin B is presented. In vitro protein biosynthesi s inhibition potency and antitumor activity were evaluated. The results ind icate that all four analogues are biologically active and could serve as ph otoaffinity reagents for the study of receptor-binding interactions of dide mnins. These analogues could also be useful in studying antitumor effects o f didemnins. (C) 2001 Elsevier Science Ltd. All rights reserved.