Synthesis and biological evaluation of pyrrolo[2,3-α]carbazole and fused indazole derivatives

Seminar by Dr. Fabrice Anizon, Clermont Université, Université Blaise Pascal, Institut de Chimie de Clermont-Ferrand, France.

Dr. Fabrice Anizon is a professor in organic chemistry at Clermont Université, Université Blaise Pascal, Institut de Chimie de Clermont-Ferrand, France. He is granted by the Åsgard-programme to meet people in university environments in Norway, interested in organic synthesis.

Topic

The Pim family of protein kinases is composed of three closely related isoforms (Pim-1, Pim-2, and Pim-3) involved in survival pathways in cancer cells. Morevover, elevated level of Pim kinases have been found in hematopoietic malignancies and solid tumors such as prostate cancer. These findings gave rise to a growing interest in the development of Pim kinase inhibitors as antitumor agents. As part of our ongoing studies aiming at developing new inhibitors of these kinases, we synthesized new heteroaromatic derivatives based on the pyrrolo[2,3-a]carbazole and indazole scaffolds. The synthesis and the biological evaluation (Pim inhibitory potency and in vitro antiproliferative activities) of these compounds as well as molecular modeling studies will be presented.

References

Suchaud, Virginie; Gavara, Laurent; Saugues, Emmanuelle; Nauton, Lionel; Thery, Vincent; Anizon, Fabrice; Moreau, Pascale. Bioorganic & Medicinal Chemistry (2013), 21(14), 4102-4111

Abstract (.pdf)

Published Feb. 24, 2014 11:44 AM - Last modified Feb. 24, 2014 11:46 AM