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Structure-activity studies of quinuclidinone analogs as anti-proliferative agents in lung cancer cell lines.

Malki A, Pulipaka AB, Evans SC, Bergmeier SC

Department of Chemistry and Biochemistry, Ohio University, Athens, OH 45701, USA.

We have synthesized and tested novel quinuclidinone analogs to assay the effects on H1299 lung cancer cell lines alone or with gamma-radiation. We have found two series of quinuclidinone analogs that act as anti-cancer agents. Of these, four interesting analogs significantly decreased cell viability in H1299 lung cancer cell lines. Two derivatives decreased cell proliferation in a dose-dependent fashion alone or in the presence of gamma-radiation. Radiosensitization increased when derivative treatment preceded radiation treatment for both derivatives. These preliminary studies show an evidence for both additive and synergistic cytotoxicity for treatment of lung cancer by these novel quinuclidinone analogs.

Published 27 January 2006 in Bioorg Med Chem Lett, 16(5): 1156-9.
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