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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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
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author 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
author_facet 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
author_sort Yin, Xiu-Juan
collection PubMed
description 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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spelling pubmed-53973922017-05-04 Synthesis and Cytotoxicity Evaluation of Tropinone Derivatives 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 Nat Prod Bioprospect Original Article 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] Springer Berlin Heidelberg 2017-03-20 /pmc/articles/PMC5397392/ /pubmed/28321792 http://dx.doi.org/10.1007/s13659-017-0124-z Text en © The Author(s) 2017 Open AccessThis article is distributed under the terms of the Creative Commons Attribution 4.0 International License (http://creativecommons.org/licenses/by/4.0/), which permits unrestricted use, distribution, and reproduction in any medium, provided you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons license, and indicate if changes were made.
spellingShingle Original Article
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
Synthesis and Cytotoxicity Evaluation of Tropinone Derivatives
title Synthesis and Cytotoxicity Evaluation of Tropinone Derivatives
title_full Synthesis and Cytotoxicity Evaluation of Tropinone Derivatives
title_fullStr Synthesis and Cytotoxicity Evaluation of Tropinone Derivatives
title_full_unstemmed Synthesis and Cytotoxicity Evaluation of Tropinone Derivatives
title_short Synthesis and Cytotoxicity Evaluation of Tropinone Derivatives
title_sort synthesis and cytotoxicity evaluation of tropinone derivatives
topic Original Article
url 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
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