title: Synthesis, topoisomerase I and II inhibitory activity, cytotoxicity, and structure-activity relationship study of hydroxylated 2,4-diphenyl-6-aryl pyridines.
abstract: A new series of 2,4-diphenyl-6-aryl pyridines containing hydroxyl group(s) at the ortho, meta, or para position of the phenyl ring were synthesized, and evaluated for topoisomerase I and II inhibitory activity and cytotoxicity against several human cancer cell lines for the development of novel anticancer agents. Structure-activity relationship study revealed that the substitution of hydroxyl group(s) increased topoisomerase I and II inhibitory activity in the order of meta > para > ortho position. Substitution of hydroxyl group on the para position showed better cytotoxicity.
authors.affiliation: College of Pharmacy, Yeungnam University, Kyongsan 712-749, Republic of Korea.
authors.forename: Radha
authors.initials: R
authors.lastname: Karki
authors.forename: Pritam
authors.initials: P
authors.lastname: Thapa
authors.forename: Mi Jeong
authors.initials: MJ
authors.lastname: Kang
authors.forename: Tae Cheon
authors.initials: TC
authors.lastname: Jeong
authors.forename: Jung Min
authors.initials: JM
authors.lastname: Nam
authors.forename: Hye-Lin
authors.initials: HL
authors.lastname: Kim
authors.forename: Younghwa
authors.initials: Y
authors.lastname: Na
authors.forename: Won-Jea
authors.initials: WJ
authors.lastname: Cho
authors.forename: Youngjoo
authors.initials: Y
authors.lastname: Kwon
authors.forename: Eung-Seok
authors.initials: ES
authors.lastname: Lee
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D003603:Cytotoxins / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D020128:Inhibitory Concentration 50; D015394:Molecular Structure; D011725:Pyridines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D059004:Topoisomerase I Inhibitors; D059005:Topoisomerase II Inhibitors
chemical_list: D000970:Antineoplastic Agents; D003603:Cytotoxins; D011725:Pyridines; D059004:Topoisomerase I Inhibitors; D059005:Topoisomerase II Inhibitors