Benzimidazole derivatives as potential dual inhibitors for PARP-1 and DHODH.
Bioorg Med Chem
; 23(15): 4669-4680, 2015 Aug 01.
Article
en En
| MEDLINE
| ID: mdl-26088338
ABSTRACT
Poly (ADP-ribose) polymerases (PARPs) play diverse roles in various cellular processes that involve DNA repair and programmed cell death. Amongst these polymerases is PARP-1 which is the key DNA damage-sensing enzyme that acts as an initiator for the DNA repair mechanism. Dihydroorotate dehydrogenase (DHODH) is an enzyme in the pyrimidine biosynthetic pathway which is an important target for anti-hyperproliferative and anti-inflammatory drug design. Since these enzymes share a common role in the DNA replication and repair mechanisms, it may be beneficial to target both PARP-1 and DHODH in attempts to design new anti-cancer agents. Benzimidazole derivatives have shown a wide variety of pharmacological activities including PARP and DHODH inhibition. We hereby report the design, synthesis and bioactivities of a series of benzimidazole derivatives as inhibitors of both the PARP-1 and DHODH enzymes.
Palabras clave
Texto completo:
1
Bases de datos:
MEDLINE
Asunto principal:
Bencimidazoles
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Poli(ADP-Ribosa) Polimerasas
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Oxidorreductasas actuantes sobre Donantes de Grupo CH-CH
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Inhibidores Enzimáticos
Idioma:
En
Revista:
Bioorg Med Chem
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2015
Tipo del documento:
Article