Giorgioni G, Ruggieri S, Di Stefano A, Sozio P, Cinque B, Di Marzio L, Santoni G, Claudi F
Dipartimento di Scienze Chimiche, Università di Camerino, Via S. Agostino 1, 62032 Camerino (MC), Italy.
Bioorg Med Chem Lett. 2008 Apr 1;18(7):2445-50. doi: 10.1016/j.bmcl.2008.02.046. Epub 2008 Mar 5.
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.
已合成抗癌药氯尼达明（LND）的多元醇衍生物。前药4、7和25表现出的水溶性增加以及它们的logP值（分别为2.19、2.55和2.54）和化学稳定性可能有利于口服给药后前药的吸收。此外，新的前药在血浆中进行酶促水解并释放LND，表明它们是体内研究的有前途的候选物。
