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Parallel Synthesis of “Click” Chalcones as Antitubulin Agents

[ Vol. 9 , Issue. 4 ]

Author(s):

Maleeruk Utsintong, Alberto Massarotti, Antonio Caldarelli and Sewan Theeramunkong   Pages 510 - 516 ( 7 )

Abstract:


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

Affiliation:

Dipartimento di Scienze del Farmaco, Universita degli Studi del Piemonte Orientale “A. Avogadro”, Largo Donegani 2, 28100 Novara, Italy.



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