title: Synthesis, antimalarial activity and cytotoxic potential of new monocarbonyl analogues of curcumin.
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 IC(50) 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.
authors.affiliation: Department of Chemistry, University of Delhi, Delhi 110007, India.
authors.forename: Sunny
authors.initials: S
authors.lastname: Manohar
authors.forename: Shabana I
authors.initials: SI
authors.lastname: Khan
authors.forename: Shamseer Kulangara
authors.initials: SK
authors.lastname: Kandi
authors.forename: Kranthi
authors.initials: K
authors.lastname: Raj
authors.forename: Guojing
authors.initials: G
authors.lastname: Sun
authors.forename: Xiaochuan
authors.initials: X
authors.lastname: Yang
authors.forename: Angie D
authors.initials: AD
authors.lastname: Calderon Molina
authors.forename: Nanting
authors.initials: N
authors.lastname: Ni
authors.forename: Binghe
authors.initials: B
authors.lastname: Wang
authors.forename: Diwan S
authors.initials: DS
authors.lastname: Rawat
mesh_terms: D000962:Antimalarials / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000494:pharmacology / Q000633:toxicity; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D003474:Curcumin / Q000031:analogs & derivatives* / Q000494:pharmacology / Q000633:toxicity; D015195:Drug Design; D006367:HeLa Cells; D006801:Humans; D010963:Plasmodium falciparum / Q000187:drug effects; D021281:Quantitative Structure-Activity Relationship
chemical_list: D000962:Antimalarials; D000970:Antineoplastic Agents; D003474:Curcumin