title: Synthesis, characterization and in vitro anticancer activity of C-5 curcumin analogues with potential to inhibit TNF-α-induced NF-κB activation.
abstract: In a search of new compounds active against cancer, synthesis of a series of C-5 curcumin analogues was carried out. The new compounds demonstrated good cytotoxicity against chronic myeloid leukemia (KBM5) and colon cancer (HCT116) cell lines. Further, these compounds were found to have better potential to inhibit TNF-α-induced NF-κB activation in comparison to curcumin, which show their potential to act as anti-inflammatory agents. Some compounds were found to show higher cytotoxicity against cancer cell lines in comparison to curcumin used as standard.
authors.affiliation: Department of Chemistry, H.N.B. Garhwal University, Srinagar Garhwal, Uttarakhand 246174, India.
authors.forename: Amit
authors.identifier: 0000-0002-7704-1789
authors.initials: A
authors.lastname: Anthwal
authors.affiliation: Department of Chemistry, H.N.B. Garhwal University, Srinagar Garhwal, Uttarakhand 246174, India.
authors.forename: Bandana K
authors.initials: BK
authors.lastname: Thakur
authors.affiliation: Department of Chemistry, H.N.B. Garhwal University, Srinagar Garhwal, Uttarakhand 246174, India.
authors.forename: M S M
authors.initials: MS
authors.lastname: Rawat
authors.affiliation: Department of Chemistry, University of Delhi, Delhi 110007, India.
authors.forename: D S
authors.initials: DS
authors.lastname: Rawat
authors.affiliation: Cytokine Research Laboratory and Pharmaceutical Development Center, Department of Experimental Therapeutics, The University of Texas M. D. Anderson Cancer Center, Houston, Texas 77030, USA.
authors.forename: Amit K
authors.initials: AK
authors.lastname: Tyagi
authors.affiliation: Cytokine Research Laboratory and Pharmaceutical Development Center, Department of Experimental Therapeutics, The University of Texas M. D. Anderson Cancer Center, Houston, Texas 77030, USA.
authors.forename: Bharat B
authors.initials: BB
authors.lastname: Aggarwal
mesh_terms: D000893:Anti-Inflammatory Agents / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D016923:Cell Death / Q000187:drug effects; D045744:Cell Line, Tumor; D003474:Curcumin / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D015536:Down-Regulation / Q000187:drug effects; D024202:Electrophoretic Mobility Shift Assay; D006801:Humans; D016328:NF-kappa B / Q000378:metabolism*; D014409:Tumor Necrosis Factor-alpha / Q000494:pharmacology*
chemical_list: D000893:Anti-Inflammatory Agents; D000970:Antineoplastic Agents; D016328:NF-kappa B; D014409:Tumor Necrosis Factor-alpha; D003474:Curcumin