Identification of Triazolothiadiazoles as Potent Inhibitors of the dCTP Pyrophosphatase 1.
J Med Chem
; 60(5): 2148-2154, 2017 03 09.
Article
en En
| MEDLINE
| ID: mdl-28145708
ABSTRACT
The dCTP pyrophosphatase 1 (dCTPase) is involved in the regulation of the cellular dNTP pool and has been linked to cancer progression. Here we report on the discovery of a series of 3,6-disubstituted triazolothiadiazoles as potent dCTPase inhibitors. Compounds 16 and 18 display good correlation between enzymatic inhibition and target engagement, together with efficacy in a cellular synergy model, deeming them as a promising starting point for hit-to-lead development.
Texto completo:
1
Base de datos:
MEDLINE
Asunto principal:
Pirofosfatasas
/
Tiadiazoles
/
Inhibidores Enzimáticos
Tipo de estudio:
Diagnostic_studies
Idioma:
En
Revista:
J Med Chem
Asunto de la revista:
QUIMICA
Año:
2017
Tipo del documento:
Article