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Devalapally, Harikrishna,Navath, Raghavendra Swamy,Yenamandra, Venkateshwarlu,Akkinepally, RaghuRam Rao,Devarakonda, Rama Krishna 대한약학회 2007 Archives of Pharmacal Research Vol.30 No.6
Anthracycline antibiotics, particularly doxorubicin and daunorubicin, have been used extensively in the treatment of human malignancies. However cardiotoxicity and multidrug resistance are significant problems that limit the clinical efficacy of such agents. Rational design to avoid these side effects includes strategies such as drug targeting and prodrug synthesis. Described here are the synthesis and preliminary biological evaluation of the enzymatically activated two new prodrugs (6 & 11) of doxorubicin. These prodrugs were designed as potential candidates for selective chemotherapy in ADEPT or PMT strategies. They are constituted of a galactose moiety, a spacer and the cytotoxic drug and they differ by the type of spacer. The prodrugs were stable in a buffer, and the in vitro studies showed good detoxification and hydrolysis kinetics. As prodrug 11 was readily hydrolyzed, this could be a valuable candidate for further development.
HariKrishna Devalapally,Raghavendra Swamy Navath,Venkateshwarlu Yenamandra,RaghuRam Rao Akkinepally,Rama Krishna Devarakonda 대한약학회 2007 Archives of Pharmacal Research Vol.30 No.6
Anthracycline antibiotics, particularly doxorubicin and daunorubicin, have been used extensively in the treatment of human malignancies. However cardiotoxicity and multidrug resistance are significant problems that limit the clinical efficacy of such agents. Rational design to avoid these side effects includes strategies such as drug targeting and prodrug synthesis. Described here are the synthesis and preliminary biological evaluation of the enzymatically activated two new prodrugs (6 & 11) of doxorubicin. These prodrugs were designed as potential candidates for selective chemotherapy in ADEPT or PMT strategies. They are constituted of a galactose moiety, a spacer and the cytotoxic drug and they differ by the type of spacer. The prodrugs were stable in a buffer, and the in vitro studies showed good detoxification and hydrolysis kinetics. As prodrug 11 was readily hydrolyzed, this could be a valuable candidate for further development.