Discovery of a nanomolar inhibitor of lung adenocarcinoma in vitro

Efficient methods for the preparation of 5′-substituted 5′-amino-5′-deoxy-N6-ureidoadenosine derivatives are described. Compounds were screened for antiproliferative activity against a panel of murine and human cell lines (L1210, CEM, and HeLa) and/or against the NCI-60. The most potent derivative inhibited the lung adenocarcinoma cell line NCI-H522 at low nanomolar concentrations (GI50 = 9.7 nM).