N-Succinyl-(β-alanyl-l-leucyl-l-alanyl-l-leucyl)doxorubicin: An Extracellularly Tumor-Activated Prodrug Devoid of Intravenous Acute Toxicity

التفاصيل البيبلوغرافية
العنوان:	N-Succinyl-(β-alanyl-l-leucyl-l-alanyl-l-leucyl)doxorubicin: An Extracellularly Tumor-Activated Prodrug Devoid of Intravenous Acute Toxicity
المؤلفون:	Fernandez, A.-M., derpoorten, K. Van, Dasnois, L., Lebtahi, K., Dubois, V., Lobl, T. J., Gangwar, S., Oliyai, C., Lewis, E. R., Shochat, D., Trouet, A.
المصدر:	Journal of Medicinal Chemistry; October 2001, Vol. 44 Issue: 22 p3750-3753, 4p
مستخلص:	Intravenous administration of N-(β-alanyl-l-leucyl-l-alanyl-l-leucyl)doxorubicin (4) induces an acute toxic reaction, killing animals in a few minutes. This results from its positive charge at physiological pH combined with its propensity to form large aggregates in aqueous solutions. Negatively charged N-capped versions of 4 such as the succinyl derivative 5 can be administered by the iv route at more than 10 times the LD50 of doxorubicin without inducing the acute toxic reaction, and they are active in vivo.
قاعدة البيانات:	Supplemental Index

الوصف
تدمد:	00222623 15204804