Synthesis and Cytotoxicity Evaluation of Tropinone Derivatives

ABSTRACT: Sixteen tropinone derivatives were prepared, and their antitumor activities against five human cancer cells (HL-60, A-549, SMMC-7721, MCF-7 and SW480) were evaluated with MTS [3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxy methoxyphenyl)-2-(4-sulfopheny)-2H-tetrazolium] assay. Most of the deriv...

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Detalles Bibliográficos
Autores principales: Yin, Xiu-Juan, Geng, Chang-An, Chen, Xing-Long, Sun, Chang-Li, Yang, Tong-Hua, Li, Tian-Ze, Zhou, Jun, Zhang, Xue-Mei, Chen, Ji-Jun
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Springer Berlin Heidelberg 2017
Materias:
Original Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5397392/
https://www.ncbi.nlm.nih.gov/pubmed/28321792
http://dx.doi.org/10.1007/s13659-017-0124-z
Descripción
Sumario:ABSTRACT: Sixteen tropinone derivatives were prepared, and their antitumor activities against five human cancer cells (HL-60, A-549, SMMC-7721, MCF-7 and SW480) were evaluated with MTS [3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxy methoxyphenyl)-2-(4-sulfopheny)-2H-tetrazolium] assay. Most of the derivatives exhibited better activities compared with tropinone at the concentration of 40 μM. Particularly, derivative 6 showed significant activities with IC(50) values of 3.39, 13.59, 6.65, 13.09 and 12.38 μM respectively against HL-60, A-549, SMMC-7721, MCF-7 and SW480 cells, which suggested more potent activities than that of cis-dichlorodiamineplatinum (DDP). GRAPHICAL ABSTRACT: [Image: see text]

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