化学
微管蛋白
康布雷他汀
化学合成
立体化学
组合化学
微管
体外
生物化学
细胞生物学
生物
作者
Natalie G. Barnes,Anthony W. Parker,Amjed A. Ahmed Mal Ullah,Patricia A. Ragazzon,John A. Hadfield
标识
DOI:10.1016/j.bmc.2020.115684
摘要
A series of combretastatin derivatives were designed and synthesised by a two-step stereoselective synthesis by use of Wittig olefination followed by Suzuki cross-coupling. Interestingly, all new compounds (2a-2i) showed potent cell-based antiproliferative activities in nanomolar concentrations. Among the compounds, 2a, 2b and 2e were the most active across three cancer cell lines. In addition, these compounds inhibited the polymerisation of tubulin in vitro more efficiently than CA-4. They caused cell cycle arrest in G2/M phase further confirming their ability to inhibit tubulin polymerisation.
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