Khan A H, Driscoll J S
J Pharm Sci. 1975 Feb;64(2):295-9. doi: 10.1002/jps.2600640222.
While pure methyl 5-(2-chloroethylamino)-5-deoxy-2,3-O-isopropylidene-beta-D-ribofuranoside hydrochloride has no L-1210 leukemia activity, a decomposed sample was found to be very active. One of several approaches taken to determine the nature of the active component involved a study of how sugar structure affects antitumor activity. A number of aminoribose derivatives were prepared and tested against the murine L-1210 and P-388 leukemia and the B-16 melanoma tumor systems. Compounds were tested as pure materials and as synthetically degraded mixtures. Both the beta-haloethyl group and a secondary amine were required for highest activity.
虽然纯的5-(2-氯乙氨基)-5-脱氧-2,3-O-异亚丙基-β-D-呋喃核糖苷盐酸甲酯没有L-1210白血病活性，但发现一个分解样品具有很强的活性。为确定活性成分的性质所采用的几种方法之一涉及研究糖结构如何影响抗肿瘤活性。制备了许多氨基核糖衍生物，并针对小鼠L-1210和P-388白血病以及B-16黑色素瘤肿瘤系统进行了测试。化合物以纯物质和合成降解混合物的形式进行测试。最高活性需要β-卤代乙基和仲胺两者。
