title: Synthesis and evaluation of novel marine bromopyrrole alkaloid-based hybrids as anticancer agents.
abstract: A series of twenty three novel hybrids of marine bromopyrrole alkaloids with chalcone, isoxazole and flavone structural features were synthesized and evaluated for in vitro anticancer activity by MTT assay against five human cancer cell lines. Among the synthesized chalcones, hybrids 4a and 4h (IC50 range: 0.18 μM-12.00 μM) showed anticancer activity against all the tested cancer cell lines. Promising cytotoxic activities were exhibited by flavones derivatives, 5a and 5b (0.41 μM-1.28 μM) against cell lines PA1 and KB403. Isoxazole hybrids, 6b-6e selectively inhibited oral and mouth cancer cell line KB403, among which 6c (IC50 = 2.45 μM) was found to be most active.
authors.affiliation: SPP School of Pharmacy and Technology Management, NMIMS University, Vile Parle, Mumbai 400056, Maharashtra, India. rajeshrane_uict@yahoo.co.in
authors.forename: Rajesh A
authors.initials: RA
authors.lastname: Rane
authors.forename: Niteshkumar U
authors.initials: NU
authors.lastname: Sahu
authors.forename: Shweta D
authors.initials: SD
authors.lastname: Gutte
authors.forename: Anand A
authors.initials: AA
authors.lastname: Mahajan
authors.forename: Chetan P
authors.initials: CP
authors.lastname: Shah
authors.forename: Pavankumar
authors.initials: P
authors.lastname: Bangalore
mesh_terms: D000470:Alkaloids / Q000737:chemistry*; D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry* / Q000494:pharmacology; D018938:Caco-2 Cells; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D002599:Chalcone / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D047309:Flavones / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D020128:Inhibitory Concentration 50; D007555:Isoxazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D061986:MCF-7 Cells; D008386:Marine Biology; D008956:Models, Chemical; D015394:Molecular Structure; D011758:Pyrroles / Q000737:chemistry*
chemical_list: D000470:Alkaloids; D000970:Antineoplastic Agents; D047309:Flavones; D007555:Isoxazoles; D011758:Pyrroles; D002599:Chalcone; C043562:flavone