Novel curcumin analogs targeting TNF-induced NF-kappaB activation and proliferation in human leukemic KBM-5 cells |
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Authors: | Zambre Ajit P Kulkarni V M Padhye Subhash Sandur Santosh K Aggarwal Bharat B |
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Institution: | Department of Medicinal Chemistry, Bharati Vidyapeeth Deemed University Poona College of Pharmacy, Pune 411 038, India. |
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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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