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

  • Bioorg Chem. 2012 Feb;40(1):67-78. doi: 10.1016/j.bioorg.2011.09.001.
Pritam Thapa  1 ,  Radha Karki  1 ,  Han Young Yoo  1 ,  Pil-Hoon Park  1 ,  Eunyoung Lee  2 ,  Kyung-Hwa Jeon  2 ,  Younghwa Na  3 ,  Won-Jea Cho  4 ,  Youngjoo Kwon  5 ,  Eung-Seok Lee  6
Affiliations
  • 1. College of Pharmacy, Yeungnam University, Kyongsan 712-749, Republic of Korea.
  • 2. College of Pharmacy, Division of Life & Pharmaceutical Sciences, Ewha Womans University, Seoul 120-750, Republic of Korea.
  • 3. College of Pharmacy, Cha University, Pochon 487-010, Republic of Korea.
  • 4. College of Pharmacy, Chonnam National University, Kwangju 500-757, Republic of Korea.
  • 5. College of Pharmacy, Division of Life & Pharmaceutical Sciences, Ewha Womans University, Seoul 120-750, Republic of Korea. Electronic address: [email protected].
  • 6. College of Pharmacy, Yeungnam University, Kyongsan 712-749, Republic of Korea. Electronic address: [email protected].
PMID: 22000119 DOI: 10.1016/j.bioorg.2011.09.001
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.

Products