Design, synthesis and docking study of 5-amino substituted indeno[1,2-c]isoquinolines as novel topoisomerase I inhibitors

  • Bioorg Med Chem. 2011 Mar 15;19(6):1924-9. doi: 10.1016/j.bmc.2011.01.064.
Daulat Bikram Khadka  1 ,  Quynh Manh Le ,  Su Hui Yang ,  Hue Thi My Van ,  Thanh Nguyen Le ,  Suk Hee Cho ,  Youngjoo Kwon ,  Kyung-Tae Lee ,  Eung-Seok Lee ,  Won-Jea Cho
Affiliations
  • 1. College of Pharmacy and Research Institute of Drug Development, Chonnam National University, Gwangju 500-757, Republic of Korea.
PMID: 21353568 DOI: 10.1016/j.bmc.2011.01.064
Abstract

Various 5-amino group-substituted indeno[1,2-c]isoquinolines 7a-f were synthesized based on the previous QSAR study as rigid structures of 3-arylisoquinolines. Amino group-substituted compounds, especially 5-piperazinyl indeno[1,2-c]isoquinoline 7f, displayed potent Topoisomerase I inhibitory activity as well as cytotoxicities against five different tumor cell lines. A Surflex-Dock docking model of 7f was also studied.