New Studying for One-pot Multicomponent Reactions to Prepare Novel Furochromone Compounds with Antitumor Activity

Abstract The refluxing of furochromone carboxaldehyde (1) and dimethyl acetylene dicarboxylate with amine derivatives namely m-nitroanilline, p-methylanilline, o-aminophenol, o-anisidine and p-anisidine to give compounds (2a-e). While the reaction of mixture of furochromone carboxaldehyde (1) with dimethyl acetylendicarboxylate in the presence of cyclohexyl isocyanide to afford compound (3). The reaction mixture of furochromone carboxaldehyde (1), cyclohexyl isocyanide with cinnamic acid, chlorocarboxylic acid and/ or benzoic acid respectively to give compounds (4a-c). Also, the condensation of furochromone carboxaldehyde (1), cyclohexyl isocyanide and o-aminophenol/and or o-phenylenediamine 5a, b respectively with chlorocarboxylic acid, carboxylic acid and cinnamic acid give compounds (6a, b – 8a, b). The addition of aldehyde with cyclohexyl isocyanide afforded compound (9) which when react with p-anisidine give compound (10). Some of the newly synthesized derivatives shows a reasonable antiproliferative activity towards liver and breast (HEPG2 & MCF7) tumor cell lines compared to traditional anticancer agents: 5-Fluorouracil & Doxorubicin. Moreover, compound 6a showed anticancer activity against NMU induced breast tumor in vivo.

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Updated: May 8, 2018 — 5:19 am