A dihydroindolizino indole derivative selectively stabilizes G-quadruplex DNA and down-regulates c-MYC expression in human cancer cells

A series of dihydroindolizino indole derivatives were synthesized and their antitumor activity, ability to selectively interact and stabilize G-quadruplex DNA were studied. Results indicate that 4-cyanophenyl linked derivative (DHII-4CPh) is superior in all aspects. It is closely followed by thiophen-2-yl (DHII-TPh) and 3-methyl-1-phenyl-1H-pyrazol-4-yl (DHII-MPhPy) linked derivatives.219