Globally cancer is a scourge: Despite advances in cancer treatment over the past decades, the prognosis of patients with cancer has improved only incrementally. There is an urgent need to develop new and effective strategies for prevention and treatment of cancer. Pyrimidine derivatives have received significant attention owing to their diverse range of biological activities such as antifungal, antitubercular, antibacterial, antiviral, anticancer and antioxidant. Concommitantly 3, 5-disubstituted isoxazolines also confer potency as antifungals and are endowed with anticancer, antiviral, insecticidal, anti-tuberculosis, antidepressant activity. We combined substituted pyrimidines with isooxazoline residues in hybrid scaffolds in a single molecular framework with enhanced and systematically attenuated biological activity. We report the synthesis of 3, 5-disubstituted isoxazolines by condensing pyrimidine based chalcones with hydroxylamine hydrochloride in ethanolic KOH. All the compounds were biologically evaluated and screened against human 60 cancer cell lines with encouraging leads. We report our ongoing investigations.

Synthesis and biological evaluation of 3, 5-disubstituted isoxazolines as potential antitumor agents

240th National Meeting (2010)

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