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Synthesis,antimalarial activity and cytotoxic potential of new monocarbonyl analogues of curcumin
Authors:Sunny Manohar  Shabana I. Khan  Shamseer Kulangara Kandi  Kranthi Raj  Guojing Sun  Xiaochuan Yang  Angie D. Calderon Molina  Nanting Ni  Binghe Wang  Diwan S. Rawat
Affiliation:1. Department of Chemistry, University of Delhi, Delhi 110007, India;2. National Centre for Natural Products Research, University of Mississippi, MS 38677, USA;3. Department of Chemistry, Center for Diagnostics and Therapeutics, and Center for Drug Design and Biotechnology, Georgia State University, Atlanta, GA 30302-4089, USA
Abstract: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 1 μM, 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.
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