title: Quinoline-azetidinone hybrids: Synthesis and in vitro antiproliferation activity against Hep G2 and Hep 3B human cell lines.
abstract: In search of new heterocyclic anticancer agents, a new quinoline-azetidinone hybrid template have been designed, synthesized and screened for their cytotoxic activity against human cancer cell lines such as Hep G2, and Hep 3B by the MTT assay and results were compared with paclitaxel, 5-fluorouracil and doxorubicin. Interestingly, some of the compounds were found significantly active against both cell lines. The compound 6f (IC50=0.04±0.01µM) exhibited potent antiproliferation activity against Hep G2 cell line, and 6j compound (IC50=0.66±0.01µM) demonstrated potent antiproliferation activity against Hep 3B cell line and provide to be more potent as cytotoxic agents than standard drugs. Morphological changes suggest the induction of apoptosis and describe the mechanism of action of these hybrid antitumor agents.
authors.affiliation: Department of Pharmaceutical Chemistry, KLE University's College of Pharmacy, Nehru Nagar, Belagavi 590010, Karnataka, India. Electronic address: sgalegaon@klepharm.edu.
authors.forename: S G
authors.initials: SG
authors.lastname: Alegaon
authors.affiliation: Department of Pharmaceutical Chemistry, KLE University's College of Pharmacy, Nehru Nagar, Belagavi 590010, Karnataka, India.
authors.forename: P
authors.initials: P
authors.lastname: Parchure
authors.affiliation: Department of Pharmaceutical Chemistry, KLE University's College of Pharmacy, Nehru Nagar, Belagavi 590010, Karnataka, India.
authors.forename: L D
authors.initials: LD
authors.lastname: Araujo
authors.affiliation: Department of Pharmaceutical Chemistry, KLE University's College of Pharmacy, Nehru Nagar, Belagavi 590010, Karnataka, India.
authors.forename: P S
authors.initials: PS
authors.lastname: Salve
authors.affiliation: Department of Pharmaceutical Chemistry, KLE University's College of Pharmacy, Nehru Nagar, Belagavi 590010, Karnataka, India.
authors.forename: K R
authors.initials: KR
authors.lastname: Alagawadi
authors.affiliation: Department of Pharmacognosy, KLE University's College of Pharmacy, Nehru Nagar, Belagavi 590010, Karnataka, India; Dr. Prabhakar Kore Basic Science Research Center, KLE University, Nehru Nagar, Belagavi 590010, Karnataka, India.
authors.forename: S S
authors.initials: SS
authors.lastname: Jalalpure
authors.affiliation: Dr. Prabhakar Kore Basic Science Research Center, KLE University, Nehru Nagar, Belagavi 590010, Karnataka, India.
authors.forename: V M
authors.initials: VM
authors.lastname: Kumbar
mesh_terms: D000634:Aminoquinolines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity; D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity; D017209:Apoptosis / Q000187:drug effects; D001384:Azetidines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity; D002522:Chlorocebus aethiops; D004317:Doxorubicin / Q000494:pharmacology; D005472:Fluorouracil / Q000494:pharmacology; D006367:HeLa Cells; D056945:Hep G2 Cells; D006801:Humans; D006860:Hydrogen Bonding; D008958:Models, Molecular; D017239:Paclitaxel / Q000494:pharmacology; D014709:Vero Cells
chemical_list: C000621529:3-chloro-1-((7-chloroquinolin-4-yl)amino)-4-(3,4-dichlorophenyl)azetidin-2-one; C000621528:3-chloro-1-((7-chloroquinolin-4-yl)amino)-4-(4-hydroxyphenyl)azetidin-2-one; D000634:Aminoquinolines; D000970:Antineoplastic Agents; D001384:Azetidines; D004317:Doxorubicin; D017239:Paclitaxel; D005472:Fluorouracil
keywords: Antiproliferation; Azetidinone; Drug likeness; Quinoline