KETONE CARBONYL-CONTAINING HYDROPHOBIC ANTITUMOR DRUG AND CONJUGATE THEREOF AS WELL AS NANO PREPARATION CONTAINING CONJUGATE, PREPARATION METHOD THEREFOR, AND APPLICATION THEREOF

摘要

The present invention provides a ketone carbonyl-containing hydrophobic antitumor drug and a conjugate thereof as well as a nano preparation containing the conjugate, a preparation method therefor, and an application thereof. The conjugate is an amphipathic pH-responsive conjugate obtained by enabling a dehydration condensation reaction between hydrazide-terminated polyethylene glycol and/or lactose hydrazide and the ketone carbonyl-introduced hydrophobic antitumor drug. The ketone carbonyl-introduced hydrophobic antitumor drug is obtained by reacting an isocyanate group in a compound containing the isocyanate group and a ketone carbonyl group with hydroxyl on a hydroxyl-containing hydrophobic antitumor drug. The hydroxyl-containing hydrophobic antitumor drug contains at least one of paclitaxel, docetaxel, paclitaxel derivatives, or docetaxel derivatives. Compared with docetaxel, the ketone carbonyl-containing hydrophobic antitumor drug and the conjugate thereof, and the nano preparation have a higher antitumor activity.