TY - JOUR
T1 - Synthesis, Pim kinase inhibitory potencies and in vitro antiproliferative activities of diversely substituted pyrrolo[2,3-a]carbazoles
AU - Akue-Gedu, Rufine
AU - Nauton, Lionel
AU - Thery, Vincent
AU - Bain, Jenny
AU - Cohen, Philip
AU - Anizon, Fabrice
AU - Moreau, Pascale
PY - 2010/9/15
Y1 - 2010/9/15
N2 - The synthesis of new pyrrolo[2,3-a]carbazole derivatives diversely substituted at the C-6 to C-9 positions is described. These compounds were tested for their kinase inhibitory potencies toward three kinases (Pim-1, Pim-2, Pim-3) as well as for their in vitro antiproliferative activities toward a human fibroblast primary culture and three human solid cancer cell lines (PC3, DU145, and PA 1). Moreover, molecular docking studies were performed to explain the enhanced inhibitory activity of the most active compound 3d. (C) 2010 Elsevier Ltd. All rights reserved.
AB - The synthesis of new pyrrolo[2,3-a]carbazole derivatives diversely substituted at the C-6 to C-9 positions is described. These compounds were tested for their kinase inhibitory potencies toward three kinases (Pim-1, Pim-2, Pim-3) as well as for their in vitro antiproliferative activities toward a human fibroblast primary culture and three human solid cancer cell lines (PC3, DU145, and PA 1). Moreover, molecular docking studies were performed to explain the enhanced inhibitory activity of the most active compound 3d. (C) 2010 Elsevier Ltd. All rights reserved.
KW - Pyrrolo[2,3-a]carbazoles
KW - Kinase inhibitors
KW - PIM inhibitors, In vitro antiproliferative activities
KW - SPECIFICITY
KW - DOCKING
U2 - 10.1016/j.bmc.2010.07.036
DO - 10.1016/j.bmc.2010.07.036
M3 - Article
C2 - 20728368
SN - 0968-0896
VL - 18
SP - 6865
EP - 6873
JO - Bioorganic & Medicinal Chemistry
JF - Bioorganic & Medicinal Chemistry
IS - 18
ER -