title: Parallel synthesis of "click" chalcones as antitubulin agents.
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.
authors.affiliation: School of Pharmaceutical Sciences, University of Phayao, 19 Moo 2 Lumpang-Phayao Road, Phayao 56000, Thailand. maleeruk.ut@up.ac.th
authors.forename: Maleeruk
authors.initials: M
authors.lastname: Utsintong
authors.forename: Alberto
authors.initials: A
authors.lastname: Massarotti
authors.forename: Antonio
authors.initials: A
authors.lastname: Caldarelli
authors.forename: Sewan
authors.initials: S
authors.lastname: Theeramunkong
mesh_terms: D045744:Cell Line, Tumor; D047188:Chalcones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D057930:Click Chemistry; D006801:Humans; D014404:Tubulin / Q000737:chemistry / Q000378:metabolism*; D050257:Tubulin Modulators / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
chemical_list: D047188:Chalcones; D014404:Tubulin; D050257:Tubulin Modulators