

8-ETHYNYLXANTHINES AS PROMISING ANTIPROLIFERATIVE AGENTS, ANGIOGENESIS INHIBITORS, AND CALCIUM CHANNEL ACTIVITY MODULATORS

Abstract
Synthetic procedures for the preparation of 8-ethynylxanthines by treating 8-bromocaffeine and 8-bromopentoxifylline with terminal acetylenes were elaborated. Certain ethynylxanthine derivatives exhibit high in vitro antiproliferative activity against a panel of cancer cell lines, matrix metalloproteinase and in vitro angiogenesis inhibitory activity. Ca2+ channel blocking and agonist activity of the synthesized ethynylxanthines was discussed based on data obtained on the H9C2, SH-SY5Y, and A7R5 cell lines.
Keywords
caffeine; xanthine; angiogenesis; calcium channel; cancer; cytotoxicity.
Latvian Institute of Organic Synthesis - Aizkraukles iela, 21, Riga, LV-1006, Latvia - hgs@osi.lv