Synthesis and Biological Activity of Fostriecin Analogs

Synthesis and Biological Activity of Fostriecin Analogs

Avila, Carolina Martins; Castro, Ilton B. D. de; Rocha, Karin J. P.; Ferreira, Carmen V.; Pilli, Ronaldo A.

Abstract:

Fostriecin (1) is a phosphate monoester produced by Streptomyces pulveraceus that displays promising antitumor activity. It has entered NCIsponsored clinical trials, but the studies were discontinued due to its storage instability and unpredictable chemical purity. In this context, more stable derivatives of fostriecin (2 and 3) have been proposed in order to evaluate the cytotoxic activity and try to understand the molecular requirements for inhibition of protein phosphatase.

Fostriecin (1) is a phosphate monoester produced by Streptomyces pulveraceus that displays promising antitumor activity. It has entered NCIsponsored clinical trials, but the studies were discontinued due to its storage instability and unpredictable chemical purity. In this context, more stable derivatives of fostriecin (2 and 3) have been proposed in order to evaluate the cytotoxic activity and try to understand the molecular requirements for inhibition of protein phosphatase.

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DOI: 10.5151/chempro-14bmos-R0166-1

Referências bibliográficas

• [1] 1 Tunac, J. B.; Graham, B. D.; Dobson, W. E. J. Antibiot. 1983, 36, 1595-1600. 2 Lewy, D. S.; Gauss, C.-M.; Soenen, D. R.; Boger, D. L. Curr. Med. Chem. 2002, 9, 2005-2032. 3 Gong, X.; An, Z.; Wang, Y.; Guan, L.; Fang, W.; Strömblad, S.; Jiang, Y.; Zhang, H. Cancer Lett. 2010, 299, 54-62.

Como citar:

Avila, Carolina Martins; Castro, Ilton B. D. de; Rocha, Karin J. P.; Ferreira, Carmen V.; Pilli, Ronaldo A.; "Synthesis and Biological Activity of Fostriecin Analogs", p-166-166. In: In Blucher Chemistry Proceedings, São Paulo, v. 1, n. 1, Setembro.2013. São Paulo: Blucher, 2013.
ISSN 23184043, DOI 10.5151/chempro-14bmos-R0166-1