title: Design, Synthesis, and In Vitro Evaluation of Novel 3, 7-Disubstituted Coumarin Derivatives as Potent Anticancer Agents.
abstract: Twenty-seven 3, 7-disubstituted coumarin derivatives were designed, synthesized, and evaluated in vitro as anticancer agents. Most of the compounds showed moderate-to-potent antiproliferative activity against K562 cells. Compounds 7b and 7d were chosen to evaluate the concentration of 50% growth inhibition (GI50 ) against SN12C, OVCAR, BxPC-3, KATO-III, T24, SNU-1, WiDr, HeLa, K562, and AGS cell lines. The most potent compound 7d was selected for further cell cycle arrest assay in the AGS cell line. The in vitro data indicated that methylation of benzimidazole moiety at the 3-position of coumarin exhibited significant enhancement of anticancer activity. This study should provide important information for further modification and optimization of coumarin derivatives as anticancer agents.
authors: Sino-American Institute of Translational Medicine, School of Pharmaceutical Sciences, Nanjing Tech University, No 5. Xinmofan Road, Nanjing, 210009, China.
authors: Yubin
authors: Y
authors: Wang
authors: Center for Biotechnology and Genomic Medicine, Medicinal College of Georgia, Georgia Regents University, 1120 15th ST, Augusta, GA, 30912, USA.
authors: Haitao
authors: H
authors: Liu
authors: Sino-American Institute of Translational Medicine, School of Pharmaceutical Sciences, Nanjing Tech University, No 5. Xinmofan Road, Nanjing, 210009, China.
authors: Peng
authors: P
authors: Lu
authors: Center for Biotechnology and Genomic Medicine, Medicinal College of Georgia, Georgia Regents University, 1120 15th ST, Augusta, GA, 30912, USA.
authors: Rui
authors: R
authors: Mao
authors: Sino-American Institute of Translational Medicine, School of Pharmaceutical Sciences, Nanjing Tech University, No 5. Xinmofan Road, Nanjing, 210009, China.
authors: Xiaojian
authors: X
authors: Xue
authors: Sino-American Institute of Translational Medicine, School of Pharmaceutical Sciences, Nanjing Tech University, No 5. Xinmofan Road, Nanjing, 210009, China.
authors: Chen
authors: C
authors: Fan
authors: Sino-American Institute of Translational Medicine, School of Pharmaceutical Sciences, Nanjing Tech University, No 5. Xinmofan Road, Nanjing, 210009, China.|Center for Biotechnology and Genomic Medicine, Medicinal College of Georgia, Georgia Regents University, 1120 15th ST, Augusta, GA, 30912, USA.
authors: Jinxiong
authors: J
authors: She
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D002453:Cell Cycle / Q000187:drug effects; D045744:Cell Line, Tumor / Q000187:drug effects; D060326:Chemistry Techniques, Synthetic; D003374:Coumarins / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor / Q000379:methods; D006801:Humans; D020014:K562 Cells / Q000187:drug effects; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D003374:Coumarins
keywords: 3, 7-disubstituted; Coumarin; anticancer activity; synthesis