Elkihel L, Gelin M, Letourneux Y
Laboratoire de Génie Protéique, Physicochimie des Substances Naturelles Université de La Rochelle, Paris, France.
Arzneimittelforschung. 1995 Feb;45(2):190-4.
A new class of chloroethyl nitrosourea analogues of cholesterol has been synthetized from the corresponding 7-amino and 7-aminoalkylcholesterol derivatives. Compounds III-V inhibited L1210 cell growth in culture much more effectively than N,N'-bis(2-chloroethyl)-N'-nitrosourea (BCNU) after 48 h incubation. Stability and cytotoxic activity of these prodrugs are promising for brain tumor treatments and as lymphotropic vectors for tumor cells spreading along the lymphatic pathways.
一类新的胆固醇氯乙基亚硝基脲类似物已从相应的7-氨基和7-氨基烷基胆固醇衍生物合成。在培养48小时后，化合物III-V比N，N'-双（2-氯乙基）-N'-亚硝基脲（BCNU）更有效地抑制培养中的L1210细胞生长。这些前药的稳定性和细胞毒性活性有望用于脑肿瘤治疗，并作为肿瘤细胞沿淋巴途径扩散的亲淋巴载体。
