Crider A M, Lamey R, Floss H G, Cassady J M, Bradner W J
J Med Chem. 1980 Aug;23(8):848-51. doi: 10.1021/jm00182a007.
Nitrosourea derivatives 18-22 which utilize either a piperidine or pyridine ring as a carrier group were synthesized and evaluated for anticancer activity. N'-(1-Benzyl-4-piperidinyl)-N-(2-chloroethyl)-N-nitosourea hydrogen maleate (19) exhibited good activity against intracranial L1210 leukemia as well as the mouse ependymoblastoma brain tumor system. Compound 19 exhibited comparable activity in the Lewis lung carcinoma system to N,N'-bis(2-chloroethyl)-N-nitrosourea. Replacement of the N-benzyl group in both the 3-piperidinyl- and 4-piperidinylnitrosoureas resulted in less active compounds in all tumor systems tested. The 3-pyridylnitrosourea 22 was inactive in the L-1210 leukemia system.
合成了以哌啶或吡啶环作为载体基团的亚硝基脲衍生物18 - 22，并对其抗癌活性进行了评估。顺丁烯二酸氢N'-(1-苄基-4-哌啶基)-N-(2-氯乙基)-N-亚硝基脲(19)对颅内L1210白血病以及小鼠室管膜母细胞瘤脑肿瘤系统表现出良好的活性。在Lewis肺癌系统中，化合物19表现出与N,N'-双(2-氯乙基)-N-亚硝基脲相当的活性。在3-哌啶基亚硝基脲和4-哌啶基亚硝基脲中，N-苄基的取代导致在所有测试的肿瘤系统中化合物活性降低。3-吡啶基亚硝基脲22在L-1210白血病系统中无活性。
