Sunday November 08 2009 | Biotechnology feed | All feeds
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Sunday November 08 2009 | Biotechnology feed | All feeds
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Novel Sulindac derivatives as candidate anti-cancer drugs There is growing evidence that NSAIDs may offer uses far exceeding their original therapeutic indications of pain and inflammation. In a recent edition of TherapeuticAdvances we have highlighted research demonstrating that the NSAID, Sulindac may target beta amyloid thus offering potential as a therapeutic intervention in Alzheimer’s disease. In addition there is growing evidence that NSAIDs may have anti-cancer activity and indeed, following their successful launch as improved analgesics, the new generation of COX-2 inhibitors are now being developed with this activity in mind. Metabolites of Sulindac, which is a non-selective COX inhibitor, are also able to inhibit cell proliferation. The mechanism of this action involves, in part, the tumorigenic Ras/Raf/MAPK pathway that is central in a large proportion of cancers due to its activation in cells bearing H-Ras mutations and consequent p21ras over-expression. Sulindac block the interaction of p21ras with the Raf kinase thus inhibiting this pathway. Thus German scientists thus synthesized a library of new Sulindac analogues. This group has recently reported the properties of 8 indene derivatives. One analogue, IND 12 was found to have a particularly exciting profile. This molecule blocked p21ras dependent signal transduction by inhibiting p21ras GTPase activity and p21ras/Raf interaction, both at significantly lower concentration than that of Sulindac. This novel series of molecules offers considerable hope for the improved treatment of cancer and deserves collaborative industrial attention in order to help speed the progress of molecules such as IND 12 towards the clinic. Link to journal abstract:
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