作者:Maleeruk Utsintong、Alberto Massarotti、Antonio Caldarelli、Sewan Theeramunkong
DOI:10.2174/1573406411309040004
日期:2013.4.1
It has been shown that some chalcones are able to inhibit tubulin polymerization, giving cytotoxicity and destruction
of tumoral vasculature. A library of 180 novel chalcone analogs has been synthesized via click chemistry and
screened for their cytotoxicity and tubulin assembly inhibition. 10 out 180 click chalcones displayed low micromolar cytotoxicity
but only compound Nf depicted antitubulin activity. While Nf displayed only micromolar potency this result
shows click-chalcones may be anti-tubulin agents and validate this strategy to search for novel active chemical entities.
研究表明,某些查耳酮能够抑制微管蛋白聚合,从而产生细胞毒性和破坏肿瘤血管。通过点击化学合成并筛选了180种新型查耳酮类似物,以评估其细胞毒性和微管组装抑制活性。在180种点击查耳酮中,有10种显示出低微摩尔级别的细胞毒性,但仅有化合物Nf表现出抗微管活性。尽管Nf仅显示出微摩尔级别的效力,但这一结果表明点击查耳酮可能作为抗微管剂,并验证了通过此策略寻找新活性化合物的方法。