Cruentaren A is a macrolide that is isolated from the myxobacterium Byssovorax cruenta, and has been shown to exhibit strong anti-proliferative activity towards various cancer cell lines via inhibition of F1F0 ATP synthase. Importantly, it was shown to be highly selective against particular cancer cells when compared to normal tissues. We previously demonstrated that Cruentaren A produces its anti-cancer activity by disrupting Hsp90/F1F0 interactions, without inducing the heat shock response (HSR). Hsp90 is the 90 kDa heat shock protein that is over-expressed in cancer cells and is responsible for the maturation of numerous client proteins. In fact, Hsp90-dependent substrates play a key role in tumor progression, which makes Hsp90 an attractive anti-cancer target. While we have previously reported the total synthesis of Cruentaren A, structure-activity relationship studies are likely to provide vital information about the importance of functionalities that have not been fully evaluated. Thus, a route has been employed that utilizes four fragments, which are then coupled in an efficient manner to yield both Cruentaren A and analogs. The synthesis and biological evaluation of Cruentaren A analogs against selected cancer cell lines will be presented.

Cruentaren A analog preparation and biological evaluation

Macromolecular Chemistry: The Second Century

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ACS Spring 2020 National Meeting & Expo

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.