title: One pot synthesis and anticancer activity of dimeric phloroglucinols.
abstract: A series of dimeric phloroglucinol compounds were synthesized in a single step using commercially available phloroglucinol and methanesulfonic acid. Based on the reported anticancer activity of plant derived dimeric phloroglucinols, these synthesized compounds were evaluated for their in vitro anti-proliferative activities against various cancer cell lines. Several compounds demonstrated in vitro cytotoxic effects across a wide array of tumor cell types. The compound 29 with pyridin-3-yl group on linker methylene and two diisovaleryl phloroglucinol moieties was found to be the most active in all the five cancer cell lines having a low IC(50) of 5.5 μM in colon cancer cell lines (HCT116).
authors.affiliation: Department of Natural Products, National Institute of Pharmaceutical Education and Research (NIPER), SAS Nagar, Punjab, India.
authors.forename: Siddheshwar K
authors.initials: SK
authors.lastname: Chauthe
authors.forename: Sandip B
authors.initials: SB
authors.lastname: Bharate
authors.forename: Giridharan
authors.initials: G
authors.lastname: Periyasamy
authors.forename: Amit
authors.initials: A
authors.lastname: Khanna
authors.forename: Kamlesh K
authors.initials: KK
authors.lastname: Bhutani
authors.forename: Prabhu D
authors.initials: PD
authors.lastname: Mishra
authors.forename: Inder P
authors.initials: IP
authors.lastname: Singh
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D019281:Dimerization; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D008698:Mesylates / Q000138:chemical synthesis* / Q000494:pharmacology; D010696:Phloroglucinol / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D008698:Mesylates; C045880:methanesulfonic acid; D010696:Phloroglucinol