Nicholas Piramal India Limited (NPIL) will be presenting their pre-clinical findings supporting the use of its novel compound(s) as anti-cancer agent. The presentation will be made at the annual meeting of the AACR-EORTC-NCI International Conference on Molecular Targets and Cancer Therapeutics, being held at Boston between November 17 – 21, 2003.
Each year, the American Association for Cancer Research (AACR), jointly with the National Cancer Institute (NCI) and the European Organization for Research and Treatment of Cancer (EORTC), brings together scientists and other professionals from around the world seeking to share the latest information in the field of molecular targets of cancer.
In pre-clinical studies conducted at Quest Institute of Life Sciences, the R&D center of Nicholas Piramal, has been found C77 novel cyclin-dependent kinase 4 (Cdk4) inhibitors as potential anticancer agents.
In NPIL’s anticancer drug discovery program, a novel series of flavones have been synthesized for evaluation against the activity of Cdk4. The scientists have identified a series of potent Cdk4-D1 inhibitors with IC50 in the range of 1.8-250 nM. These compounds also exhibit 50 to 600-fold better selectivity towards Cdk4-D1, than to Cdk2-E. Further, these compounds showed potent antiproliferative effects against 10 human cancerous cell lines, with an average IC50 of 200-1000 nM. Of these, three compounds have been extensively evaluated for their antiproliferative effects in 20 additional cell lines, clonogenic assays, antitumor efficacy in vivo, toxicity, specificity towards kinases and activation of caspase-3. These compounds were 20 to 30-fold more potent than cis-plastin in their antiproliferative effects against 16 human cancerous cell lines.
Ajay Piramal, chairman of Nicholas Piramal, echoed the sentiment, saying: “The world is currently witnessing critical innovations and new knowledge in cancer research. New therapies are available or in development. We are honoured to be invited to share our work and represent the research capabilities of the nation at this prestigious global forum.”