Effects of altering the electronics of 2-methoxyestradiol on cell proliferation, on cytotoxicity in human cancer cell cultures, and on tubulin polymerization
AB Edsall, AK Mohanakrishnan, D Yang…
文献索引:Edsall, Allison B.; Mohanakrishnan, Arasambattu K.; Yang, Donglai; Fanwick, Philip E.; Hamel, Ernest; Hanson, Arthur D.; Agoston, Gregory E.; Cushman, Mark Journal of Medicinal Chemistry, 2004 , vol. 47, # 21 p. 5126 - 5139
A series of new analogues of 2-methoxyestradiol (1) were synthesized to further elucidate the relationships between structure and activity. The compounds were designed to diminish the potential for metabolic deactivation at positions 2 and 17 and were analyzed as inhibitors of tubulin polymerization and for cytotoxicity. 17α-Methyl-β-estradiol (30), 2- propynyl-17α-methylestradiol (39), 2-ethoxy-17-(1'-methylene) estra-1, 3, 5 (10)-triene-3- ...