title: Synthesis and Cytotoxic Evaluation of Monocarbonyl Analogs of Curcumin as Potential Anti-Tumor Agents.
abstract: Preclinical Research A series of mono-carbonyl curcumin analogs with different substituents at the 4/4'-position of the phenyl group were synthesized and screened for in vitro cytotoxicity against a panel of human cancer cell lines using a methyl thiazolyl tetrazolium assay. Several of the curcumin analogs, especially B114, exhibited a wide-spectrum of anti-tumor properties in all tested cell lines, indicating their potential in as anti-cancer lead compounds. Further toxicity testing in the NRK-52E kidney cell line revealed that the analogs A111, A113, and B114 had comparable or higher safety than curcumin. These data suggested that the introduction of appropriate substituents in the 4/4'-positions could be a promising approach for curcumin-based drug design.
authors: The First Affiliated Hospital of Soochow University, Suzhou, Jiangsu, People's Republic of China.|Department of Orthopedic Surgery, The First Affiliated Hospital, Wenzhou Medical University, Wenzhou, Zhejiang, People's Republic of China.
authors: Zheer
authors: Z
authors: Pan
authors: Department of Orthopedic Surgery, The First Affiliated Hospital, Wenzhou Medical University, Wenzhou, Zhejiang, People's Republic of China.
authors: Chengwei
authors: C
authors: Chen
authors: Department of Orthopedic Surgery, The First Affiliated Hospital, Wenzhou Medical University, Wenzhou, Zhejiang, People's Republic of China.
authors: Yeli
authors: Y
authors: Zhou
authors: Department of Orthopedic Surgery, The First Affiliated Hospital, Wenzhou Medical University, Wenzhou, Zhejiang, People's Republic of China.
authors: Feng
authors: F
authors: Xu
authors: The First Affiliated Hospital of Soochow University, Suzhou, Jiangsu, People's Republic of China.
authors: Yaozeng
authors: Y
authors: Xu
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D003474:Curcumin / Q000031:analogs & derivatives*; D004354:Drug Screening Assays, Antitumor; D006367:HeLa Cells; D056945:Hep G2 Cells; D006801:Humans; D015394:Molecular Structure
chemical_list: D000970:Antineoplastic Agents; D003474:Curcumin
keywords: anti-tumor activity; monocarbonyl curcumin analogs; synthesis