Preparation and evaluation of new brominated paclitaxel analogues
Titel:
Preparation and evaluation of new brominated paclitaxel analogues
Auteur:
Jiang, Yi Lin, Hai-Xia Li, Ming Wu, Bei-Li Chen, Jian-Min
Verschenen in:
Journal of Asian natural products research
Paginering:
Jaargang 7 (2005) nr. 3 pagina's 231-236
Jaar:
2005-06
Inhoud:
Two diastereomers of 2'',3''-dibromo-7-epi-10-deacetylcephalomannine, 4 and 5, have been synthesized, purified and identified for evaluation as antitumour drugs. The cytotoxicity of the two diastereomers, assessed in cell culture against MCF-7 breast cancer, A549 lung cancer and A2780 ovarian cancer, was slightly stronger than that of paclitaxel. The cytotoxicity of 5 outweighs that of 4. In the light of the difference in cytotoxicity between the two diastereomers, we can assume that the differing configurations of C-2'' and C-3'' of the two diastereomers may result in different bioactive conformations in solution and, consequently, different biologically relevant conformations for binding to tubulin/microtubules — a matter we are studying further.