Evaluation of PNU-159682 antibody drug conjugates (ADCs).
Bioorg Med Chem Lett
; 30(24): 127640, 2020 12 15.
Article
em En
| MEDLINE
| ID: mdl-33127540
ABSTRACT
PNU-159682 is a highly potent secondary metabolite of nemorubicin belonging to the anthracycline class of natural products. Due to its extremely high potency and only partially understood mechanism of action, it was deemed an interesting starting point for the development of a new suite of linker drugs for antibody drug conjugates (ADCs). Structure activity relationships were explored on the small molecule which led to six linker drugs being developed for conjugation to antibodies. Herein we describe the synthesis of novel PNU-159682 derivatives and the subsequent linker drugs as well as the corresponding biological evaluations of the small molecules and ADCs.
Palavras-chave
Texto completo:
1
Bases de dados:
MEDLINE
Assunto principal:
Doxorrubicina
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Imunoconjugados
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Antineoplásicos
Limite:
Animals
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Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Assunto da revista:
BIOQUIMICA
/
QUIMICA
Ano de publicação:
2020
Tipo de documento:
Article