title: Design, synthesis, and antitumor evaluation of 2,4,6-triaryl pyridines containing chlorophenyl and phenolic moiety.
abstract: We have designed and synthesized a series of 2,4,6-triaryl pyridine derivatives containing chlorophenyl and phenolic moeity at 2- and 4- position of the central pyridine, respectively, resulting in a total of 42 compounds. They were evaluated for topoisomerase I and II inhibitory activities as well as cytotoxicities against several human cancer cell lines. Most compounds showed better topoisomerase II inhibitory activity compared to topoisomerase I inhibitory activity. Compounds 19, 20, 26-28, and 47-50 especially showed stronger topo II inhibitory activity than etoposide.
authors.affiliation: College of Pharmacy, Yeungnam University, 214-1 Dae-dong, Gyeongsan 712-749, Republic of Korea.
authors.forename: Pritam
authors.initials: P
authors.lastname: Thapa
authors.forename: Radha
authors.initials: R
authors.lastname: Karki
authors.forename: Minho
authors.initials: M
authors.lastname: Yun
authors.forename: Tara Man
authors.initials: TM
authors.lastname: Kadayat
authors.forename: Eunyoung
authors.initials: E
authors.lastname: Lee
authors.forename: Han Byeol
authors.initials: HB
authors.lastname: Kwon
authors.forename: Younghwa
authors.initials: Y
authors.lastname: Na
authors.forename: Won-Jea
authors.initials: WJ
authors.lastname: Cho
authors.forename: Nam Doo
authors.initials: ND
authors.lastname: Kim
authors.forename: Byeong-Seon
authors.initials: BS
authors.lastname: Jeong
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; D060326:Chemistry Techniques, Synthetic; D004264:DNA Topoisomerases, Type I / Q000737:chemistry / Q000378:metabolism; D004250:DNA Topoisomerases, Type II / Q000737:chemistry / Q000378:metabolism; D015195:Drug Design; D006801:Humans; D008958:Models, Molecular; D010636:Phenols / Q000737:chemistry*; D011487:Protein Conformation; D011725:Pyridines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D000970:Antineoplastic Agents; D010636:Phenols; D011725:Pyridines; D004264:DNA Topoisomerases, Type I; D004250:DNA Topoisomerases, Type II