| 摘要 |
Clinical utility of chemotherapy agents is limited by dose-dependent systemic toxicity and emergence of resistant tumor cell lines. The present invention provides derivatives of chemotherapeutic agents which can overcome these limitations. Reaction of a parent drug with glutaraldehyde in aqueous solution followed by ethanolamine yields a product which exhibits enhanced antitumor cytotoxicity and overcomes resistance developed against the parent drug. The derivative compounds of the invention achieve therapeutic effects comparable to those of the parent drugs but at much lower doses, thereby reducing undesirable toxic side effects. The most preferred derivative is glutaraldehyde-modified doxorubicin. Most preferred are methods of treatment for subjects suffering from cancer which comprise administration of glutaraldehyde-modified doxorubicin. |
