Wampler G L, Nassiri S K, Hsiao Y Y, Bardos T J, Regelson W
Cancer Res. 1975 Aug;35(8):1903-6.
1,3,4,6-Tetra-O-acetyl-2-(di-2-chloroethyl)amino-2-deoxy-D-glucopyranose is active against L1210 leukemia, giving over 100% increased life-span at optimal dose. Against P388 leukemia, it gives 200% increased life-span with long-term survivors. The compound is most active when given i.p., but shows some activity when given s.c. than p.o., and is more potent (therapeutic and toxic effect) than mechlorethamine on both a molar and a mg basis. Of importance, the schedule dependency for the administration of 1,3,4,6-tetra-O-acetyl-2-(di-2-chloroethyl)amino-2-deoxy-D-glucopyranose in L1210 leukemia differs from most alkylating agents in that it is best given by multiple daily injections rather than as a single large injection on Day 1. This characteristic can be attributed to the amino-glucose moiety.
1,3,4,6-四-O-乙酰基-2-（二-2-氯乙基）氨基-2-脱氧-D-吡喃葡萄糖对L1210白血病具有活性，在最佳剂量下可使寿命延长超过100%。对P388白血病，它可使寿命延长200%，并有长期存活者。该化合物腹腔注射时活性最强，但皮下注射时也有一定活性，口服活性较弱，在摩尔和毫克基础上，其效力（治疗和毒性作用）均比氮芥更强。重要的是，1,3,4,6-四-O-乙酰基-2-（二-2-氯乙基）氨基-2-脱氧-D-吡喃葡萄糖在L1210白血病中的给药方案依赖性与大多数烷化剂不同，即最好每日多次注射，而不是在第1天单次大剂量注射。这一特性可归因于氨基葡萄糖部分。
