Synthesis and in vitro activity of some methylenomycin analogs.

A cationic cyclopentannelation reaction has afforded a very simple route to a wide variety of methylenomycin analogs. The antibacterial activity of these readily accessible synthetic compounds parallels that of naturally occurring methylenomycin A. The in vitro antitumor activity of the synthetics assayed using human nasopharyngeal carcinoma (KB) cells is particularly promising.