Biology Department Seminar

Hypoxia-inducible factor-1alpha (HIF-1alpha) is a critical regulatory protein of cellular response to hypoxia, and regulates the transcription of many genes involved in key aspects of cancer biology, including immortalization, maintenance of stem cell pools, cellular dedifferentiation, vascularization and invasion / metastasis. HIF-1alpha has been implicated in the regulation of genes involved in angiogenesis e.g. VEGF and is associated with tumor progression. In last decade, the over expression of HIF-1alpha has been demonstrated in many common human cancers and has emerged as a validated target for anticancer drug discovery. In the present talk design, synthesis and anticancer potential of pyridyl-pyrimidine based novel molecules will be discussed in brief.1-5
References: 1) Kumar S., Joshi K., Deore V., Bhonde M., Yewalkar N., Amol P, Rathos M., Almeida A., Parikh S., Dagia N. “Pyridyl derivatives, their preparation and use” WO 2009019656 A1. 2) Yewalkar N, Deore V, Padgaonkar A, Manohar S, Sahu B, Kumar P, Badhwar AJ, Joshi K, Sharma S, Kumar S. Development of novel inhibitors targeting HIF-1alpha towards anticancer drug discovery. Bioorg. Med. Chem. Lett. 2010, 20, 6426-6429. 3) Roychowdhury A, Sharma R & Kumar S. Recent advances in the discovery of small molecule mTOR inhibitors. Future Medicinal Chemistry. 2010, 2 (10), 1577-1589. 4) Deore V, Yewalkar N, Bhatia D, Desai N, Gupte RD, Dadarkar SS, Jadhav MG, Tannu AA, Bhatt P, Nemmani K, Vishwakarma R, Sharma S, Roychowdhury A, M. Dagia N, Bhonde M and Kumar S. Synthesis and Therapeutic Evaluation of Pyridyl Based Novel mTOR Inhibitors. Bioorg. Med. Chem. Lett. 2009, 19, 2949-2952. 5) Lohar M, Mundada R, Bhonde M, Padgaonkar A, Deore V, Yewalkar N, Bhatia D, Rathos M, Joshi K, Vishwakarma R & Kumar S. Design and Synthesis of Novel Furoquinoline Based Inhibitors of Multiple Targets in the PI3K/Akt-mTOR Pathway. Bioorg. Med. Chem. Lett. 2008, 18, 3603-3609.