Indoloquinolines as scaffolds for the design of potent G-quadruplex ligands

Indoloquinolines are natural Alkaloids with known affinity to DNA and antiproliferative activity against bacteria, parasites, and Cancer cells. Due to their non-chiral skeleton, their total synthesis is easy to achieve and throughout the years, many derivatives have been studied for their potential as drugs. Herein we review the indoloquinolines and bioisosters that have been designed, synthesised, and evaluated for their selective binding to G-quadruplex nucleic acid structures, as well as the reported effects in Cancer cells. The data collected so far strongly suggest that indoloquinolines are good scaffolds for the development of drugs and probes targeting the G-quadruplex structures, but they also show that this scaffold is still underexplored.

Benzofuroquinoline; Cancer; DNA; G-quadruplex; Indolo[3,2-b]quinoline; indolo[3,2-c]quinoline.