Concise Synthesis and Biological Evaluation of the Pyrrolo[4,3,2-de]quinoline Core of the Lymphostin Family

The efficient synthesis of the pyrrolo­[4,3,2-de]­quinoline core of the lymphostin family (compound 1) has been accomplished in 7 steps and 18.6% overall yield, providing an efficient method for the total synthesis and structural modification of the lymphostin family. Compound 1 showed potent inhibitory activities against PI3K/mTOR in the nanomolar range and activity against human colorectal cancer cell lines comparable to that of oxaliplatin, which could be recognized as a novel lead compound for cancer therapy.