Syntheses of Anti-Lung Cancer Agents( II )

This project is aimed to synthesize a new series of ALK inhibitors and identify drug candidate for the treatment of lung cancer. For 1st year result, we synthesized a series of compounds as anti-lung cancer agents. 8 of them displayed substantial antiproliferative activity against lung A549 (KRAS mutant), H1975 (EGFR resistant), and H2228 (ALK positive) cancer cell lines, better than two FDA approval drugs (Crizotinib, Ceritinib) and third-generation ALK inhibitors (Lorlatinib). In the in vivo efficacy evaluation, lead compound showed superior activity than Crizotinib. In this year proposal, we will continuously synthesize and find a drug candidate as anti-ALK lung cancer agent with good PK profile and in vivo efficacy.