Chiu F T, Chang Y H, Ozkan G, Zon G, Fichter K C, Phillips L R
J Pharm Sci. 1982 May;71(5):542-51. doi: 10.1002/jps.2600710517.
N- and O-Triorganosilylated compounds related to various anticancer agents were synthesized for evaluation as potential anticancer prodrugs. 1H-NMR and UV kinetic measurements of hydrolytic desilylation were used to correlate relative rates of structural unmasking with steric bulk about the silicon reaction center. The tert-butyldimethylsilyl ester of chlorambucil and a number of O- triorganosilylated carbamate derivatives of nor-nitrogen mustard showed significant activity against P-388 lymphocytic leukemia in mice.
合成了与各种抗癌剂相关的N-和O-三有机硅烷化化合物，以评估其作为潜在抗癌前药的可能性。利用1H-NMR和水解脱硅反应的紫外动力学测量来关联结构去掩蔽的相对速率与硅反应中心周围的空间位阻。苯丁酸氮芥的叔丁基二甲基硅酯和一些去氮芥的O-三有机硅烷化氨基甲酸酯衍生物对小鼠P-388淋巴细胞白血病显示出显著活性。
