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

Pavel Arsenyan, Jelena Vasiljeva, Ilona Domracheva, Iveta Kanepe-Lapsa
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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.

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