Pharmachemie B.v.

Ruben G Leenders

Dick De Vos

Johan W Scheeren

Hidde J Haisma

Eric Wilhelmus Damen

Pieter H Houba

Hendricus B De Bont

A paclitaxel prodrug has a paclitaxel portion coupled to a cleavable N-(aliphatic or aromatic)-O-glycosyl carbamate spacer group, and can be administered orally, topically or by injection to provide an anti-tumor effect, the prodrug being activated by a hydrolizing enzyme, an endogeneous enzyme or an exogeneous enzyme.

Paclitaxel prodrugs, method for preparation as well as their use in

Anthracycline derivatives are disclosed which are coupled to an enzymatically cleavable N-phenyl-O-glycosyl carbamate spacer group, which derivatives are represented by the formula ##STR1## as well as the acid addition salts thereof. Further the synthesis of these derivatives and their use, alone or in combination with enzymes or antibody enzyme conjugates are disclosed.

Anthracycline prodrugs, method for preparation as well as their use in

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Nijmegen, Netherlands

Ruben G Leenders