Concise Synthesis and\nBiological Evaluation of the\nPyrrolo[4,3,2-<i>de</i>]quinoline Core of the Lymphostin\nFamily

The\nefficient synthesis of the pyrrolo[4,3,2-<i>de</i>]quinoline\ncore of the lymphostin family (compound <b>1</b>) has been accomplished\nin 7 steps and 18.6% overall yield, providing\nan efficient method for the total synthesis and structural modification\nof the lymphostin family. Compound <b>1</b> showed potent inhibitory\nactivities against PI3K/mTOR in the nanomolar range and activity against\nhuman colorectal cancer cell lines comparable to that of oxaliplatin,\nwhich could be recognized as a novel lead compound for cancer therapy.