An efficient synthesis of argifin: a natural product chitinase inhibitor with chemotherapeutic potential

Reference:

Dixon, M. J., Andersen, O. A., van Aalten, D. M. F. and Eggleston, I. M., 2005. An efficient synthesis of argifin: a natural product chitinase inhibitor with chemotherapeutic potential. Bioorganic & Medicinal Chemistry Letters, 15 (21), pp. 4717-4721.

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Official URL:

http://dx.doi.org/10.1016/j.bmcl.2005.07.068

Abstract

The first synthesis of the cyclopentapeptide family 18 chitinase inhibitor argifin has been achieved by a combination of solid phase and solution chemistry. Synthetic argifin is a nanomolar inhibitor of chitinase B1 from Aspergillus fumigatus and the high-resolution X-ray structure of the synthesized material in complex with the same enzyme is identical to that previously obtained for the natural product.

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