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

被引：70

作者：

Zambre, Ajit P.

Kulkarni, V. M.

Padhye, Subhash ^{[1
]}

Sandur, Santosh K.

Aggarwal, Bharat B.

机构：

[1] Univ Poona, Drug Design & Mol Med Grp, Dept Chem, Pune 411007, Maharashtra, India

[2] Bharati Vidyapeeth Deemed Univ, Poona Coll Pharm, Dept Med Chem, Pune 411038, Maharashtra, India

[3] Univ Texas, MD Anderson Canc Ctr, Cytokine Res Lab, Dept Expt Therapeut, Houston, TX 77030 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2006年 / 14卷 / 21期

关键词：

curcumin; NF-kappa B; thiosemicarbazone; copper; knoevenagel condensation;

D O I：

10.1016/j.bmc.2006.06.056

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

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-kappa B 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. (c) 2006 Elsevier Ltd. All rights reserved.

引用

页码：7196 / 7204

页数：9

共 27 条

[1] Transition metal complexes of phenanthrenequinone thiosemicarbazone as potential anticancer agents: synthesis, structure, spectroscopy, electrochemistry and in vitro anticancer activity against human breast cancer cell-line, T47D [J].