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

Authors

  • Pavel Arsenyan Latvian Institute of Organic Synthesis, 21 Aizkraukles St., Riga LV-1006, Latvia
  • Jelena Vasiljeva Latvian Institute of Organic Synthesis, 21 Aizkraukles St., Riga LV-1006, Latvia
  • Ilona Domracheva Latvian Institute of Organic Synthesis, 21 Aizkraukles St., Riga LV-1006, Latvia
  • Iveta Kanepe-Lapsa Latvian Institute of Organic Synthesis, 21 Aizkraukles St., Riga LV-1006, Latvia

DOI:

https://doi.org/10.1007/5418

Keywords:

caffeine, xanthine, angiogenesis, calcium channel, cancer, cytotoxicity.

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.

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Published

2020-07-10

Issue

Vol. 56 No. 6 (2020): Heterocyclic сompounds in medicinal chemistry

Section

Original Papers