title: Synthesis and biological evaluation of a novel class of coumarin derivatives.
abstract: In this study, several novel coumarin derivatives, 7-hydroxy-2-oxo-2H-chromene-3-carboxyl-Trp-Trp-AA-OBzl compounds, were designed and synthesized as potential anticancer agents. Their in vitro cytotoxic activities were evaluated using methylthiazoltetrazolium (MTT) assay. The anti-tumor activity of the newly coumarin derivatives was determined in a S180 bearing mouse model and some of the compounds demonstrated tumor growth inhibition similar to the positive control, doxorubicin. Compared to doxorubicin, most of the compounds exhibited enhanced immunologic function suggesting a relatively minor toxic effect. The intercalation of the coumarin derivatives synthesized with calf thymus (CT) DNA was also studied.
authors.affiliation: College of Pharmaceutical Sciences, Capital Medical University, Beijing 100069, PR China.
authors.forename: Hong
authors.initials: H
authors.lastname: Li
authors.affiliation: Department of Physiology, Key Laboratory for Neurodegenerative Disorders of the Ministry of Education, Capital Medical University, Beijing 100069, PR China.
authors.forename: Xiaomin
authors.initials: X
authors.lastname: Wang
authors.affiliation: College of Pharmaceutical Sciences, Capital Medical University, Beijing 100069, PR China.
authors.forename: Guichao
authors.initials: G
authors.lastname: Xu
authors.affiliation: College of Pharmaceutical Sciences, Capital Medical University, Beijing 100069, PR China.
authors.forename: Li
authors.initials: L
authors.lastname: Zeng
authors.affiliation: College of Pharmaceutical Sciences, Capital Medical University, Beijing 100069, PR China.
authors.forename: Kai
authors.initials: K
authors.lastname: Cheng
authors.affiliation: School of Pharmaceutical Sciences, Peking University, Beijing 100191, PR China.
authors.forename: Pengchao
authors.initials: P
authors.lastname: Gao
authors.affiliation: College of Pharmaceutical Sciences, Capital Medical University, Beijing 100069, PR China.
authors.forename: Qing
authors.initials: Q
authors.lastname: Sun
authors.affiliation: College of Pharmaceutical Sciences, Capital Medical University, Beijing 100069, PR China.
authors.forename: Wei
authors.initials: W
authors.lastname: Liao
authors.affiliation: College of Pharmaceutical Sciences, Capital Medical University, Beijing 100069, PR China. Electronic address: jwzhang2006@163.com.
authors.forename: Jianwei
authors.initials: J
authors.lastname: Zhang
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology / Q000627:therapeutic use; D002417:Cattle; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D002942:Circular Dichroism; D003374:Coumarins / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use; D004247:DNA / Q000737:chemistry / Q000378:metabolism; D004317:Doxorubicin / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D006801:Humans; D051379:Mice; D009369:Neoplasms / Q000188:drug therapy; D014183:Transplantation, Heterologous
chemical_list: D000970:Antineoplastic Agents; D003374:Coumarins; D004317:Doxorubicin; D004247:DNA; C427203:calf thymus DNA
keywords: Amino acid; Anti-tumor; Coumarin; Cytotoxicity; Peptide