title: Synthesis and anticancer activity of novel curcumin-quinolone hybrids.
abstract: A number of new curcumin-quinolone hybrids were synthesised from differently substituted 3-formyl-2-quinolones and vanillin and their in vitro cytotoxicity was determined on a panel of representative cell lines (A549, MCF7, SKOV3 and H460) using MTT assay. The most potent compound 14, was analysed for its mode of action using various cell biology experiments. SKOV3 cells treated with compound 14 showed distorted cell morphology under phase contrast imaging and induction of apoptosis was confirmed by Annexin V/PE assay. Further experiments on generation of reactive oxygen species (ROS) and cell cycle analysis revealed that these hybrids induce apoptosis by ROS generation and arrest cell cycle progression in S and G2/M phase.
authors.affiliation: Department of Medicinal Chemistry, Sri Ramachandra University, Chennai 600 116, India.
authors.forename: Saiharish
authors.initials: S
authors.lastname: Raghavan
authors.affiliation: Department of Human Genetics, Sri Ramachandra University, Chennai 600 116, India.
authors.forename: Prasath
authors.initials: P
authors.lastname: Manogaran
authors.affiliation: Department of Medicinal Chemistry, Sri Ramachandra University, Chennai 600 116, India. Electronic address: drkrishna2011@gmail.com.
authors.forename: Krishna Kumari
authors.initials: KK
authors.lastname: Gadepalli Narasimha
authors.affiliation: Department of Medicinal Chemistry, Sri Ramachandra University, Chennai 600 116, India.
authors.forename: Balasubramanian
authors.initials: B
authors.lastname: Kalpattu Kuppusami
authors.affiliation: Department of Medicinal Chemistry, Sri Ramachandra University, Chennai 600 116, India.
authors.forename: Palanivelu
authors.initials: P
authors.lastname: Mariyappan
authors.affiliation: Department of Human Genetics, Sri Ramachandra University, Chennai 600 116, India.
authors.forename: Anjana
authors.initials: A
authors.lastname: Gopalakrishnan
authors.affiliation: Department of Human Genetics, Sri Ramachandra University, Chennai 600 116, India. Electronic address: ganeshv@sriramachandra.edu.in.
authors.forename: Ganesh
authors.initials: G
authors.lastname: Venkatraman
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects; D002453:Cell Cycle / Q000187:drug effects; D045744:Cell Line, Tumor; D003474:Curcumin / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology*; D006801:Humans; D009369:Neoplasms / Q000188:drug therapy / Q000378:metabolism; D015363:Quinolones / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D017382:Reactive Oxygen Species / Q000378:metabolism
chemical_list: D000970:Antineoplastic Agents; D015363:Quinolones; D017382:Reactive Oxygen Species; D003474:Curcumin
keywords: Annexin-V; Cell cycle analysis; Curcumin–quinolone hybrids; MTT assay