Studies toward the duocarmycin prodrugs for the antibody prodrug therapy approach.
Tetrahedron Lett
; 50(24): 2933-2935, 2009 Jun 01.
Article
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| MEDLINE
| ID: mdl-20160897
ABSTRACT
A tricyclic precursor for the synthesis of the prodrugs of pro-1,2,9,9a-tetrahydrocyclopropa[c]benz-[e]indole-4-one tetramethoxyindolecarboxamide (CBI-TMI) was prepared using the ring-closing metathesis approach. The tricyclic intermediate was converted to an advanced precursor of a CBI-TMI prodrug equipped with a linker presumably suitable for activation using the aldolase catalytic antibody 38C2. An attempted 38C2-catalyzed two-step activation of the hydroxy-pro-CBI intermediate involving retro-aldol and the ß-elimination reactions was also examined.
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Colección:
01-internacional
Banco de datos:
MEDLINE
Idioma:
En
Revista:
Tetrahedron Lett
Año:
2009
Tipo del documento:
Article