title: Synthesis and biological evaluation of novel curcuminoid derivatives.
abstract: Curcuminoids have been reported to possess multiple bioactivities, such as antioxidant, anticancer and anti-inflammatory properties. Three novel series of curcuminoid derivatives (11a-h, 15a-h and 19a-d) with enhanced bioactivity have been synthesized. Among the synthesized compounds, 11b exhibited the most significant activity with an MIC of 0.5 µM /mL against selected medically important Gram-positive cocci (S. aureus and S. viridans) and Gram-negative bacilli (E. coli and E. cloacae). The derivatives exhibited remarkable results in an antioxidant test with an IC50 2.4- to 9.3-folder smaller than curcuminoids. With respect to antiproliferative activity against Hep-G2, LX-2, SMMC7221 and MDA-MB-231, the derivatives exhibited an effect stronger than curcuminoids with an IC50 ranging from 0.18 to 4.25 µM.
authors.affiliation: Department of Applied Chemistry, Marine College, Shandong University, Weihai 264209, China. yakun_cao@163.com.
authors.forename: Ya-Kun
authors.initials: YK
authors.lastname: Cao
authors.affiliation: Department of Environmental Engineering, School of Marine Science and Technology, Harbin Institute of Technology, Weihai 264209, China. lihuijing@iccas.ac.cn.
authors.forename: Hui-Jing
authors.initials: HJ
authors.lastname: Li
authors.affiliation: Department of Applied Chemistry, Marine College, Shandong University, Weihai 264209, China. zhifangdl@163.com.
authors.forename: Zhi-Fang
authors.initials: ZF
authors.lastname: Song
authors.affiliation: Department of Applied Chemistry, Marine College, Shandong University, Weihai 264209, China. LYchemlh@hotmail.com.
authors.forename: Yang
authors.initials: Y
authors.lastname: Li
authors.affiliation: Department of Applied Chemistry, Marine College, Shandong University, Weihai 264209, China. huaiqy06@sdu.edu.cn.
authors.forename: Qi-Yong
authors.initials: QY
authors.lastname: Huai
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D000975:Antioxidants / Q000138:chemical synthesis* / Q000494:pharmacology; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D003474:Curcumin / Q000031:analogs & derivatives*; D004925:Escherichia / Q000145:classification / Q000187:drug effects; D056945:Hep G2 Cells; D006801:Humans; D013210:Staphylococcus / Q000145:classification / Q000187:drug effects
chemical_list: D000900:Anti-Bacterial Agents; D000970:Antineoplastic Agents; D000975:Antioxidants; D003474:Curcumin