1.
Bioorg Med Chem Lett
; 14(12): 3057-61, 2004 Jun 21.
Artigo
em Inglês
| MEDLINE
| ID: mdl-15149644
RESUMO
The synthesis of a novel series of 1,7-annulated indolocarbazoles 2 and 16 is described. These compounds were found to be potent cyclin dependent kinase inhibitors with good antiproliferative activity against two human carcinoma cell lines. These inhibitors also arrested tumor cells at the G1 phase and inhibited pRb phosphorylation.
Assuntos
Quinases Ciclina-Dependentes/antagonistas & inibidores , Indóis/síntese química , Inibidores de Proteínas Quinases/síntese química , Antineoplásicos/síntese química , Antineoplásicos/farmacologia , Linhagem Celular Tumoral , Quinases Ciclina-Dependentes/metabolismo , Inibidores do Crescimento/síntese química , Inibidores do Crescimento/farmacologia , Humanos , Indóis/farmacologia , Inibidores de Proteínas Quinases/farmacologia
2.
Bioorg Med Chem Lett
; 13(14): 2261-7, 2003 Jul 21.
Artigo
em Inglês
| MEDLINE
| ID: mdl-12824014
RESUMO
The synthesis and CDK inhibitory properties of a series of indolo[6,7-a]pyrrolo[3,4-c]carbazoles is reported. In addition to their potent CDK activity, the compounds display antiproliferative activity against two human cancer cell lines. These inhibitors also effect strong G1 arrest in these cell lines and inhibit Rb phosphorylation at Ser780 consistent with inhibition of cyclin D1/CDK4.