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.

中文翻译：

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8-Ethynylxanthines作为有前途的抗增殖药，血管生成抑制剂和钙通道活性调节剂

阐述了通过用末端乙炔处理8-溴咖啡因和8-溴戊氧茶碱来制备8-乙炔基黄嘌呤的合成方法。某些乙炔基黄嘌呤衍生物对一组癌细胞具有较高的体外抗增殖活性，基质金属蛋白酶和体外血管生成抑制活性。基于在H9C2，SH-SY5Y和A7R5细胞系上获得的数据，讨论了合成的乙炔基黄嘌呤的Ca ²⁺通道阻滞和激动剂活性。