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Novel curcumin analogs targeting TNF-induced NF-kappaB activation and proliferation in human leukemic KBM-5 cells
Authors:Zambre Ajit P  Kulkarni V M  Padhye Subhash  Sandur Santosh K  Aggarwal Bharat B
Institution:Department of Medicinal Chemistry, Bharati Vidyapeeth Deemed University Poona College of Pharmacy, Pune 411 038, India.
Abstract:Novel curcumin analogs were synthesized using Knoevenagel condensation to convert enolic diketones of curcumin into non-enolizable ones and Schiff bases were prepared using a bioactive thiosemicarbazide pharmacophore. Copper(II) conjugates of all synthesized ligands were prepared and structurally characterized as well as evaluated for their potential of inhibiting TNF-induced NF-kappaB activation and proliferation in human leukemic KBM-5 cells wherein compound 13 was found to be more potent than curcumin. Compounds were further examined on other tumor cell lines such as Jurkat, H1299, and MM1, respectively.
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