SYNTHESIS OF GEM-BISPHOSPHONIC DOXORUBICIN CONJUGATES

Authors
FABULET O STURTZ G
Citation
O. Fabulet et G. Sturtz, SYNTHESIS OF GEM-BISPHOSPHONIC DOXORUBICIN CONJUGATES, Phosphorus, sulfur and silicon and the related elements, 101(1-4), 1995, pp. 225-234
Citations number
15
Categorie Soggetti
Chemistry Inorganic & Nuclear
Journal title
Phosphorus, sulfur and silicon and the related elements → ACNP
ISSN journal
10426507
Volume
101
Issue
1-4
Year of publication
1995
Pages
225 - 234
Database
ISI
SICI code
1042-6507(1995)101:1-4<225:SOGDC>2.0.ZU;2-R
Abstract
Four gem-bisphosphonic doxorubicin conjugates are prepared by coupling the amino function of doxorubicin with the activated carboxylic funct ions of 3,3-bis(diethylphosphono)propanoic acid 2, 4,4-bis(diethylphos phono)butanoic acid 3, and (R + arbonyl)-2-amino-4,4-bis(diethylphosph ono)butanoic acid 6. The last compound provides two epimers which are separated by chromatography. Sodium salts are obtained. These original products participate in a biological study about a delivery-targeting concept of antineoplastic agents in bone cancer therapy, with the ass istance of gem-bisphosphonic building blocks.