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.
Keywords: Antitubulinic agent, Cancer, Chalcone analogs, Click chemistry, Cytotoxicity, Tubulin
Rights & PermissionsPrintExport