Novel curcumin analogs targeting TNF-induced NF-kappaB activation and proliferation in human leukemic KBM-5 cells.
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.
Zambre
Ajit P
AP
Department of Medicinal Chemistry, Bharati Vidyapeeth Deemed University Poona College of Pharmacy, Pune 411 038, India.
Kulkarni
V M
VM
Padhye
Subhash
S
Sandur
Santosh K
SK
Aggarwal
Bharat B
BB
D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects*; D003474:Curcumin / Q000031:analogs & derivatives* / Q000494:pharmacology; D004354:Drug Screening Assays, Antitumor; D004563:Electrochemistry; D006801:Humans; D007938:Leukemia / Q000473:pathology*; D016328:NF-kappa B / Q000378:metabolism*; D013057:Spectrum Analysis / Q000379:methods; D014409:Tumor Necrosis Factor-alpha / Q000502:physiology*
D016328:NF-kappa B; D014409:Tumor Necrosis Factor-alpha; D003474:Curcumin