SYNTHESIS AND CHEMICAL-PROPERTIES OF A SERIES OF DOXORUBICIN ENAMINOMALONYL-BETA-ALANINE DERIVATIVES

Authors
SEITZ DE EZCURRA JE GUTTMAN DL
Citation
De. Seitz et al., SYNTHESIS AND CHEMICAL-PROPERTIES OF A SERIES OF DOXORUBICIN ENAMINOMALONYL-BETA-ALANINE DERIVATIVES, Tetrahedron letters, 36(9), 1995, pp. 1413-1416
Citations number
14
Categorie Soggetti
Chemistry Inorganic & Nuclear
Journal title
Tetrahedron letters → ACNP
ISSN journal
00404039
Volume
36
Issue
9
Year of publication
1995
Pages
1413 - 1416
Database
ISI
SICI code
0040-4039(1995)36:9<1413:SACOAS>2.0.ZU;2-9
Abstract
A series of doxorubicin enaminomalonyl-beta-alanine derivatives 1a-e h as been synthesized as potential drug-linker domains of an antibody dr ug conjugate. The release of doxorubicin from these enamide derivative s under acidic and neutral conditions has been evaluated. Two activate d esters, 6a and 6c, suitable for coupling to a monoclonal antibody ha ve been prepared.