Colchicine analogues in which an azo group is incorporated into a molecule containing the key pharmacophore of colchicine, have found particular utility as switchable tubulin binding chemotherapeutics. Combretastatin is a related compound containing a stilbene fragment that shows different bioactivity for the cis and trans isomers. We have performed cell assays on 17 new compounds structurally related to a previously reported azo-analogue of combretastatin. One of these compounds showed enhanced potency against HeLa (IC₅₀ = 0.11 μM) and H157 cells (IC₅₀ = 0.20 μM) for cell studies under 400 nm irradiation and the highest photoactivity (IC₅₀ with irradiation/IC₅₀ in dark = 550). We have performed docking and physicochemical studies of this new compound (7). Kinetic studies in water reveal a longer half-life for the cis isomer of 7 which may be one factor responsible for the better IC₅₀ values in cell assays and the improved photoresponsive behavior.

已发现将秋水仙碱类似物（其中偶氮基团掺入含有秋水仙碱的关键药效​​团的分子中）特别可用作可切换的微管蛋白结合化学疗法。Combretastatin是一种相关化合物，其中含有1,2-二苯乙烯片段，该片段显示出对顺式和反式异构体不同的生物活性。我们已经对与先前报道的康维他汀的偶氮类似物在结构上相关的17种新化合物进行了细胞测定。这些化合物之一对 400 nm辐射下的细胞研究具有最高的HeLa（IC ₅₀  = 0.11μM）和H157细胞（IC ₅₀ = 0.20μM）的效力，并且具有最高的光活度（IC ₅₀与辐射/ IC ₅₀在黑暗中= 550）。我们已经对该新化合物（7）进行了对接和理化研究。水中的动力学研究表明，顺式异构体7的半衰期更长，这可能是细胞分析中更好的IC ₅₀值和改善的光响应行为的一个因素。