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Total synthesis and biological evaluation of simplified aplyronine analogues as synthetically tractable anticancer agents

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Abstract

The aplyronines are a family of highly cytotoxic marine natural products with potential application in targeted cancer chemotherapy. To address the severe supply issue, function-oriented molecular editing of their macrolactone scaffold led to the design of a series of simplified aplyronine analogues. Enabled by a highly convergent aldol-based route, the total synthesis of four analogues was achieved, with a significant improvement in step economy versus previous compounds, and their cancer cell growth inhibition in the HeLa cell line was determined. The modular strategy presented offers a means for significantly shortening their chemical synthesis to facilitate the continued development of this promising class of anticancer agent.

Graphical abstract: Total synthesis and biological evaluation of simplified aplyronine analogues as synthetically tractable anticancer agents

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Article information


Submitted
20 Nov 2019
Accepted
03 Jan 2020
First published
03 Jan 2020

Chem. Commun., 2020, Advance Article
Article type
Communication

Total synthesis and biological evaluation of simplified aplyronine analogues as synthetically tractable anticancer agents

T. R. Pettigrew, R. J. Porter, S. J. Walsh, M. P. Housden, N. Y. S. Lam, J. S. Carroll, J. S. Parker, D. R. Spring and I. Paterson, Chem. Commun., 2020, Advance Article , DOI: 10.1039/C9CC09050A

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