Glycosyl and polyalcoholic prodrugs of lonidamine.

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作者信息

Giorgioni G, Ruggieri S, Di Stefano A, Sozio P, Cinque B, Di Marzio L, Santoni G, Claudi F

机构信息

Dipartimento di Scienze Chimiche, Università di Camerino, Via S. Agostino 1, 62032 Camerino (MC), Italy.

出版信息

Bioorg Med Chem Lett. 2008 Apr 1;18(7):2445-50. doi: 10.1016/j.bmcl.2008.02.046. Epub 2008 Mar 5.

DOI:10.1016/j.bmcl.2008.02.046

PMID:18321702

Abstract

Polyhydric alcohol derivatives of the anticancer agent lonidamine (LND) have been synthesized. The increased water solubility showed by prodrugs 4, 7, and 25 together with their logP values (2.19, 2.55, and 2.54, respectively) and chemical stability might be beneficial for prodrugs absorption after oral administration. Moreover, the new prodrugs undergo enzymatic hydrolysis in plasma and release LND demonstrating that they are promising candidates for in vivo investigations.

摘要