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Tumor protease activated prodrugs of phosphoramide mustard analogs with toxification and detoxification functionalities
Tumor protease activated prodrugs of phosphoramide mustard analogs with toxification and detoxification functionalities
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机译:具有酰胺化和解毒功能的磷酰胺芥末类似物的肿瘤蛋白酶激活前药
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摘要
The composition, synthesis, and applications of tumor associated protease activated prodrugs of phosphoramide mustard, isophosphoramide mustard and analogs with detoxification functionalities are described. These drugs release a cytotoxic phosphoramide mustard analog following activation by tumor associated proteases and esterases. The general structure for these drugs is: ##STR1## Wherein R1 is a beta-X- ethyl-amino group which may optionally bear substituents on the nitrogen or carbon atoms; wherein X is a good leaving group such as a halogen; R2 is a beta- X-ethyl-amino group which may optionally bear substituents on the nitrogen or carbon atoms; or an amino group (NH.sub.2) which may optionally be substituted. Wherein A is a benzyloxy derivative with one or more acyloxy or acylamino groups in para or ortho portions relative to the phosphoester; and wherein the acyloxy or acylamino groups are not (substituted or unsubstituted) p-guanidino-benzoyloxy groups or p- guanidino-benzoylamino groups.
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机译:描述了磷酰胺芥末,异磷酰胺芥末和具有解毒功能的类似物的肿瘤相关蛋白酶激活的前药的组成,合成和应用。这些药物在被肿瘤相关的蛋白酶和酯酶激活后释放出细胞毒性磷酰胺芥末类似物。这些药物的一般结构是:其中R1是β-X-乙基-氨基,它可以任选地在氮或碳原子上带有取代基。其中X是良好的离去基团,例如卤素; R 2是β-X-乙基-氨基,它可以任选地在氮或碳原子上带有取代基;或可以任选被取代的氨基(NH 2)。其中A是相对于磷酸酯在对位或邻位具有一个或多个酰氧基或酰氨基的苄氧基衍生物;并且其中所述酰氧基或酰氨基不是(取代或未取代的)对胍基-苯甲酰氧基或对胍基-苯甲酰氨基。
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