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US 2014/0155336 A1Published application
Water-soluble camptothecin derivative, pharmaceutical composition and use thereof
AssigneeHunan Fangshenghuamei Medical Tech. Co. Ltd.
InventorsWenqiang Zhou, Jing Deng
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Abstract
The present invention relates to a water soluble derivative of camptothecin and preparation method thereof, the derivative having a structure of formula I and being appropriate in water solubility, and having anti-cancer activity and stability of lactonic ring. The present invention also relates to a method for synthesizing the compound and medical use of the compound.
Claims20
A water-soluble camptothecin derivative, comprising
- a compound of Formula I
- and pharmaceutically acceptable salts thereof:
- wherein M represents hydroxyl or thiol, A represents ribose or deoxyribose or ribose derivative and is attached to a phosphorus atom via an oxygen of an hydroxyl group
A camptothecin derivative comprising a chemical structure of Formula II:
- wherein R1 represents hydrogen, C1-C4 acyl, or an enzymatically reactive moiety;
- R2 and R3 are the same or different, and independently represents hydrogen, halo, hydroxyl, alkoxy group, or an enzymatically reactive moiety;
- B is hydrogen, optionally substituted thymine, optionally substituted adenine, optionally substituted cytosine, optionally substituted guanine, optionally substituted uracil, 5-fluorouricil, 5-aza-cytosine, 2-fluoroadenine, 2-chloroadenine, or 3,4,7,8-tetrahydroimidazo[1,3]-diazepin-8-ol;
- or
- B is a heteroaromatic or heteroalicyclic group other than adenine, thymidine, cytosine or guanine and preferably has from 1 to 3 mono-cyclic or fused-rings and 1 to 3 N, O or S atoms.
2 more elements
Dependencies are inferred from the claim text.