Design and synthesis of 4-amino-2-phenylquinazolines as novel topoisomerase I inhibitors with molecular modeling

4-Amino-2-phenylquinazolines 7 were designed as bioisosteres of 3-arylisoquinolinamines 6 that were energy minimized to provide stable conformers. Interestingly, the 2-phenyl ring of 4-amino-2-phenylquinazolines was parallel to the quinazoline ring and improved their DNA intercalation ability in the DNA-topo I complex.


Thanh Nguyen Le, Su Hui Yang, Daulat Bikram Khadka, Hue Thi My Van, Suk Hee Cho, Youngjoo Kwon, Eung-Seok Lee, Kyung-Tae Lee, Won-Jea Cho
July 15, 2011
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