Synthesis, antimalarial activity and cytotoxic potential of new monocarbonyl analogues of curcumin

• Published in: Bioorganic & medicinal chemistry letters 2013-01, Vol.23 (1), p.112-116
• Main Authors: Manohar, Sunny, Khan, Shabana I., Kandi, Shamseer Kulangara, Raj, Kranthi, Sun, Guojing, Yang, Xiaochuan, Calderon Molina, Angie D., Ni, Nanting, Wang, Binghe, Rawat, Diwan S.
• Format: Article
• Language: English
• Subjects: Anticancer; Antimalarial; antimalarials; Antimalarials - chemical synthesis; Antimalarials - pharmacology; Antimalarials - toxicity; Antineoplastic Agents - chemical synthesis; Antineoplastic Agents - pharmacology; Antineoplastic Agents - toxicity; Cell Line, Tumor; Cell Survival - drug effects; chemistry; Curcumin; Curcumin - analogs & derivatives; Curcumin - pharmacology; Curcumin - toxicity; Cytotoxicity; doxorubicin; Drug Design; Food and Drug Administration; HeLa cell line; HeLa Cells; Humans; inhibitory concentration 50; Plasmodium falciparum; Plasmodium falciparum - drug effects; Quantitative Structure-Activity Relationship; screening
• ISSN: 0960-894X; 1464-3405
• DOI: 10.1016/j.bmcl.2012.11.004

A series of novel monocarbonyl analogues of curcumin have been designed, synthesized and tested for their activity against Molt4, HeLa, PC3, DU145 and KB cancer cell lines. Six of the analogues showed potent cytotoxicity towards these cell lines with IC50 values below 1μM, which is better than doxorubicin, a US FDA approved drug. Several analogues were also found to be active against both CQ-resistant (W2 clone) and CQ-sensitive (D6) strains of Plasmodium falciparum in an in-vitro antimalarial screening. This level of activity warrants further investigation of the compounds for development as anticancer and antimalarial agents.