title: Synthesis of biscoumarin and dihydropyran derivatives with promising antitumor and antibacterial activities.
abstract: Two series of biscoumarin (1-3) and dihydropyran (4-12) derivatives were successfully synthesized as new antitumor and antibacterial agents. The molecular structures of four representative compounds 2, 4, 7 and 10 were confirmed by single crystal X-ray diffraction study. The synthesized compounds (1-12) were evaluated for their antitumor activities against human intestinal epithelial adenocarcinoma cell line (HuTu80), mammary adenocarcinoma cell line (4T1) and pancreatic cancer cell line (PANC1) and antibacterial activities against one drug-sensitive Staphylococcus aureus (S. aureus ATCC 29213) strain and three MRSA strains (MRSA XJ 75302, Mu50, USA 300 LAC). The further mechanism study demonstrated that the most potent compound 1 could obviously inhibit the proliferation of cancer cells via the mechanism to induce apoptosis.
authors.affiliation: School of Chemical Engineering, The Key Laboratory for Surface Engineering and Remanufacturing in Shaanxi Province, Xi'an University, Xi'an 710065, China.
authors.forename: Jing
authors.initials: J
authors.lastname: Li
authors.affiliation: Institute of Chinese Materia Medica, China Academy of Chinese Medical Sciences, Beijing 100700, China; Beijing Chao-Yang Hospital, Capital Medical University, Beijing 100020, China.
authors.forename: Yun-Peng
authors.initials: YP
authors.lastname: Sui
authors.affiliation: Department of Blood Transfusion, Xijing Hospital, The Fourth Military Medical University, Xi'an 710032, China.
authors.forename: Jia-Jia
authors.initials: JJ
authors.lastname: Xin
authors.affiliation: Graduate School of China Academy of Chinese Medical Sciences, Beijing 100700, China.
authors.forename: Xin-Liang
authors.initials: XL
authors.lastname: Du
authors.affiliation: School of Chemical Engineering, The Key Laboratory for Surface Engineering and Remanufacturing in Shaanxi Province, Xi'an University, Xi'an 710065, China.
authors.forename: Jiang-Tao
authors.initials: JT
authors.lastname: Li
authors.affiliation: Institute of Chinese Materia Medica, China Academy of Chinese Medical Sciences, Beijing 100700, China.
authors.forename: Hai-Ru
authors.initials: HR
authors.lastname: Huo
authors.affiliation: Institute of Chinese Materia Medica, China Academy of Chinese Medical Sciences, Beijing 100700, China.
authors.forename: Hai
authors.initials: H
authors.lastname: Ma
authors.affiliation: Institute of Chinese Materia Medica, China Academy of Chinese Medical Sciences, Beijing 100700, China.
authors.forename: Wei-Hao
authors.initials: WH
authors.lastname: Wang
authors.affiliation: Institute of Chinese Materia Medica, China Academy of Chinese Medical Sciences, Beijing 100700, China.
authors.forename: Hai-Yu
authors.initials: HY
authors.lastname: Zhou
authors.affiliation: Institute of Chinese Materia Medica, China Academy of Chinese Medical Sciences, Beijing 100700, China.
authors.forename: Hong-Dan
authors.initials: HD
authors.lastname: Zhan
authors.affiliation: Institute of Chinese Materia Medica, China Academy of Chinese Medical Sciences, Beijing 100700, China.
authors.forename: Zhu-Ju
authors.initials: ZJ
authors.lastname: Wang
authors.affiliation: Institute of Chinese Materia Medica, China Academy of Chinese Medical Sciences, Beijing 100700, China.
authors.forename: Chun
authors.initials: C
authors.lastname: Li
authors.affiliation: Institute of Chinese Materia Medica, China Academy of Chinese Medical Sciences, Beijing 100700, China. Electronic address: fsui@icmm.ac.cn.
authors.forename: Feng
authors.initials: F
authors.lastname: Sui
authors.affiliation: Department of Neurosurgery, Xijing Hospital, The Fourth Military Medical University, Xi'an 710032, China. Electronic address: sjwklixia@sina.com.
authors.forename: Xia
authors.initials: X
authors.lastname: Li
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D017209:Apoptosis / Q000187:drug effects*; D016190:Carboplatin / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D003374:Coumarins / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D018360:Crystallography, X-Ray; D006801:Humans; D020128:Inhibitory Concentration 50; D008826:Microbial Sensitivity Tests; D008958:Models, Molecular; D011714:Pyrans / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013211:Staphylococcus aureus / Q000187:drug effects*
chemical_list: D000900:Anti-Bacterial Agents; D000970:Antineoplastic Agents; D003374:Coumarins; D011714:Pyrans; C073813:3,4-dihydropyran; D016190:Carboplatin
keywords: Antibacterial; Antitumor; Biscoumarin; Dihydropyran