862469-79-2Relevant academic research and scientific papers
Design, synthesis, and biological evaluation of 1,3-diarylisoquinolines as novel topoisomerase I catalytic inhibitors
Khadka, Daulat Bikram,Park, Seojeong,Jin, Yifeng,Han, Jinhe,Kwon, Youngjoo,Cho, Won-Jea
supporting information, p. 200 - 215 (2017/11/27)
With a goal of identifying potent topoisomerase (topo) inhibitor, the C4-aromatic ring of the anticancer agent, 3,4-diarylisoquinolone, was strategically shifted to design 1,3-diarylisoquinoline. Twenty-two target compounds were synthesized in three simple and efficient steps. The 1,3-diarylisoquinolines exhibited potent anti-proliferative effects on cancer cells but few compounds spared non-cancerous cells. Inhibition of topo I/IIα-mediated DNA relaxation by several derivatives was greater than that by camptothecin (CPT)/etoposide even at low concentration (20 μM). In addition, these compounds had little or no effect on polymerization of tubulin. A series of biological evaluations performed with the most potent derivative 4cc revealed that the compound is a non-intercalative topo I catalytic inhibitor interacting with free topo I. Collectively, the potent cytotoxic effect on cancer cells including the drug resistance ones, absence of lethal effect on normal cells, and different mechanism of action than topo I poisons suggest that the 1,3-diarylisoquinolines might be a promising class of anticancer agents worthy of further pursuit.
Synthesis, in vitro and in vivo evaluation of 3-arylisoquinolinamines as potent antitumor agents
Yang, Su Hui,Van, Hue Thi My,Le, Thanh Nguyen,Khadka, Daulat Bikram,Cho, Suk Hee,Lee, Kyung-Tae,Chung, Hwa-Jin,Lee, Sang Kook,Ahn, Chang-Ho,Lee, Young Bok,Cho, Won-Jea
scheme or table, p. 5277 - 5281 (2010/10/21)
In the search for potent water-soluble 3-arylisoquinolines, several 3-arylisoquinolinamines were designed and synthesized. Various substituted 3-arylisoquinolinamines exhibited strong cytotoxic activity against eight different human cancer cell lines. In
