Methods of preparing CPT-esters are described. The methods include using at least one acid in the esterification reactions or acylation reactions of camptothecins.
描述了制备CPT酯的方法。这些方法包括在紫杉醇的酯化反应或酰化反应中使用至少一种酸。
Liposomal prodrugs comprising derivatives of camptothecin and methods of treating cancer using these prodrugs
申请人:The Stehlin Foundation For Cancer Research
公开号:US06352996B1
公开(公告)日:2002-03-05
Derivatives of camptothecin as represented by the general formula:
are described, wherein when R1 is H, R. is a C2-C4 alkyl group, a C6-C15 alkyl group, a C3-C8 cycloalkyl group, a C2-C15 alkenyl group or a C2-C15 epoxy group; and when R2 is a nitro group or an amino group, R1 is a C1-C15 alkyl group, a C1-C15 alkenyl group, a C3-C8 cycloalkyl group, or an epoxy group. Liposomal prodrugs including these specific derivatives of camptothecin restrained by a liposomal delivery system are also described. Processes for making these prodrugs and for using them in cancer treatment are also disclosed.
Hydrated crystalline camptothecin esters, such as crystalline aliphatic ester hydrates of camptothecin, pharmaceutical compositions containing crystalline aliphatic ester hydrates of camptothecin, methods of treating a cancer or malignant tumor using the crystalline camptothecin ester hydrates and methods of making the same are described.