Substituent effects within the DNA binding subunit of CBI analogues of the duocarmycins and CC-1065.
Bioorg Med Chem Lett
; 11(15): 2021-4, 2001 Aug 06.
Article
em En
| MEDLINE
| ID: mdl-11454471
ABSTRACT
A series of CBI analogues of the duocarmycins and CC-1065 exploring substituent effects within the first indole DNA binding subunit are detailed. Substitution at the indole C5 position led to cytotoxic potency enhancements that are > or =1000-fold, providing simplified analogues containing a single DNA binding subunit that are more potent (IC(50)=2-3 pM) than CBI-TMI, duocarmycin SA, or CC-1065.
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Base de dados:
MEDLINE
Assunto principal:
Pirróis
/
Pirrolidinonas
/
DNA
/
Leucomicinas
/
Antibióticos Antineoplásicos
Idioma:
En
Ano de publicação:
2001
Tipo de documento:
Article