Parallel Synthesis of “Click” Chalcones as Antitubulin Agents

Author(s): Maleeruk Utsintong, Alberto Massarotti, Antonio Caldarelli, Sewan Theeramunkong.

Journal Name: Medicinal Chemistry

Volume 9 , Issue 4 , 2013

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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

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Article Details

Year: 2013
Page: [510 - 516]
Pages: 7
DOI: 10.2174/1573406411309040004
Price: $58

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