Author/Authors :
Guoxin Zhu، نويسنده , , Scott Conner، نويسنده , , Xun Zhou، نويسنده , , Chuan Shih، نويسنده , , Harold B. Brooks، نويسنده , , Eileen Considine، نويسنده , , Jack A. Dempsey، نويسنده , , Cathy Ogg، نويسنده , , Bharvin Patel، نويسنده , , Richard M. Schultz، نويسنده , , Charles D. Spencer، نويسنده , , Beverly Teicher، نويسنده , , Scott A. Watkins، نويسنده ,
Abstract :
A novel series of pyrrolo[3,4-c] carbazoles fused with a quinolinyl/isoquinolinyl moiety were synthesized and their D1/CDK4 inhibitory and antiproliferative activity were evaluated. Compound 8H, 14H-isoquinolinyl[6,5-a]-pyrrolo[3,4-c]carbazole-7,9-dione (1d) was found to be a highly potent D1/CDK4 inhibitor with an IC50 of 69 nM. Compound 1d also inhibited tumor cell growth, arrested tumor cells in G1 phase and inhibited pRb phosphorylation.
