Novel curcumin analogs targeting TNF-induced NF-kappaB activation and proliferation in human leukemic KBM-5 cells

  • Bioorg Med Chem. 2006 Nov 1;14(21):7196-204. doi: 10.1016/j.bmc.2006.06.056.
Ajit P Zambre  1 ,  V M Kulkarni ,  Subhash Padhye ,  Santosh K Sandur ,  Bharat B Aggarwal
Affiliations
  • 1. Department of Medicinal Chemistry, Bharati Vidyapeeth Deemed University Poona College of Pharmacy, Pune 411 038, India.
PMID: 16843665 DOI: 10.1016/j.bmc.2006.06.056
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.