Diverse heterocyclic scaffolds as dCTP pyrophosphatase 1 inhibitors. Part 1: Triazoles, triazolopyrimidines, triazinoindoles, quinoline hydrazones and arylpiperazines.
Bioorg Med Chem Lett
; 27(16): 3897-3904, 2017 08 15.
Article
en En
| MEDLINE
| ID: mdl-28687206
ABSTRACT
A high-throughput screening campaign using a commercial compound library (ChemBridge DiverSET) revealed diverse chemotypes as inhibitors of the human dCTP pyrophosphatase 1 (dCTPase). Triazole, triazolopyrimidine, triazinoindole, quinoline hydrazone and arylpiperazine hits were clustered, confirmed by IC50 determinations, and their preliminary structure-activity-relationships (SAR) and ligand efficiency scores are discussed in this letter.
Texto completo:
1
Banco de datos:
MEDLINE
Asunto principal:
Pirofosfatasas
/
Inhibidores Enzimáticos
/
Compuestos Heterocíclicos
Límite:
Humans
Idioma:
En
Año:
2017
Tipo del documento:
Article