title: 2,4-Diaryl-5,6-dihydro-1,10-phenanthroline and 2,4-diaryl-5,6-dihydrothieno[2,3-h] quinoline derivatives for topoisomerase I and II inhibitory activity, cytotoxicity, and structure-activity relationship study.
abstract: Designed and synthesized thirty-two 2,4-diaryl-5,6-dihydro-1,10-phenanthroline and 2,4-diaryl-5,6-dihydrothieno[2,3-h] quinoline derivatives as rigid analogs of 2,4,6-trisubstituted pyridines were evaluated for topoisomerase I and II inhibitory activities as well as cytotoxicities against several human cancer cell lines. Structure-activity relationship study showed that [2,2';6',2"]-terpyridine skeleton is important for the cytotoxicity against several human cancer cell lines.
authors: College of Pharmacy, Yeungnam University, Kyongsan 712-749, Republic of Korea.
authors: Pritam
authors: P
authors: Thapa
authors: College of Pharmacy, Yeungnam University, Kyongsan 712-749, Republic of Korea.
authors: Radha
authors: R
authors: Karki
authors: College of Pharmacy, Yeungnam University, Kyongsan 712-749, Republic of Korea.
authors: Han Young
authors: HY
authors: Yoo
authors: College of Pharmacy, Yeungnam University, Kyongsan 712-749, Republic of Korea.
authors: Pil-Hoon
authors: PH
authors: Park
authors: College of Pharmacy, Division of Life & Pharmaceutical Sciences, Ewha Womans University, Seoul 120-750, Republic of Korea.
authors: Eunyoung
authors: E
authors: Lee
authors: College of Pharmacy, Division of Life & Pharmaceutical Sciences, Ewha Womans University, Seoul 120-750, Republic of Korea.
authors: Kyung-Hwa
authors: KH
authors: Jeon
authors: College of Pharmacy, Cha University, Pochon 487-010, Republic of Korea.
authors: Younghwa
authors: Y
authors: Na
authors: College of Pharmacy, Chonnam National University, Kwangju 500-757, Republic of Korea.
authors: Won-Jea
authors: WJ
authors: Cho
authors: College of Pharmacy, Division of Life & Pharmaceutical Sciences, Ewha Womans University, Seoul 120-750, Republic of Korea. Electronic address: ykwon@ewha.ac.kr.
authors: Youngjoo
authors: Y
authors: Kwon
authors: College of Pharmacy, Yeungnam University, Kyongsan 712-749, Republic of Korea. Electronic address: eslee@yu.ac.kr.
authors: Eung-Seok
authors: ES
authors: Lee
mesh_terms: D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D004264:DNA Topoisomerases, Type I / Q000737:chemistry* / Q000378:metabolism; D004250:DNA Topoisomerases, Type II / Q000737:chemistry* / Q000378:metabolism; D004354:Drug Screening Assays, Antitumor; D004789:Enzyme Activation / Q000187:drug effects; D006801:Humans; D010618:Phenanthrolines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D011804:Quinolines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D013329:Structure-Activity Relationship; D059004:Topoisomerase I Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D059005:Topoisomerase II Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology
chemical_list: D010618:Phenanthrolines; D011804:Quinolines; D059004:Topoisomerase I Inhibitors; D059005:Topoisomerase II Inhibitors; D004264:DNA Topoisomerases, Type I; D004250:DNA Topoisomerases, Type II; C025205:1,10-phenanthroline