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Synthesis and antitumor activity evaluation of novel 1-phenyl-1 benzofuran/benzothiopheneyl methenecycloalkane derivatives
Pages: 497-500,510
Year: Issue:  9
Journal: Qilu Pharmaceutical Affairs

Keyword:  1-phenyl-1-benzofuran/benzothiopheneylmethenecycloalkane derivativesVascular disrupting agentsAn-titumor activitySynthesis;
Abstract: Objective To synthesize and evaluate antitumor activity of a series of novel 1-phenyl-1-benzofuran/benzothiopheneyl methenecycloalkane derivatives. Methods Compounds 2a ~ 2c were synthesized via condensation, Mcmurry reaction,using substituted salicylaldehydes or 2-hydroxyacetophenone( 4a~4c)as starting materials;using salicyl-aldehyde(6a)or 2-hydroxyacetophenone(6b)as starting materials,after treated with dimethylthiocarbamoyl chloride,rear-rangement,hydrolysis,condensation,Mcmurry reaction to yield 3a~3b. The antitumor activity on human CEM cells was as-sessed by MTT method.Results The structures of 5 target compounds synthesized in this paper were confirmed by 1 H-NMR,13 C-NMR and HRMS.Compounds 3a~3b showed similar antitumor activity against human leukemia cells CEM to that of lead compound 1,but all target compounds were less effective than that of Combretastatin A-4(CA-4).Conclusion Replacement the B-ring of lead compound 1 with benzothiophene resulted in the retention of antitumor activity.
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