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Synthesis and biological evaluation of a new series of 1-aryl-3-[4-(pyridin-2-ylmethoxy)phenyl]urea derivatives as new anticancer agents
The diaryl ureas are very important fragments in medicinal chemistry. By means of computer-aided design, 1-aryl-3-[4-(pyridin-2-ylmethoxy)phenyl]urea derivatives were designed and synthesized, and evaluated for their antiproliferative activity against A549, HCT-116, PC-3 cancer cell lines, and HL770...
Autores principales: | , , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
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Springer US
2020
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7232929/ https://www.ncbi.nlm.nih.gov/pubmed/32427204 http://dx.doi.org/10.1007/s00044-020-02554-z |
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author | Feng, Jian Li, Tai Liang, Shishao Zhang, Chuanming Tan, Xiaoyu Ding, Ning Wang, Xin Liu, Xiaoping Hu, Chun |
author_facet | Feng, Jian Li, Tai Liang, Shishao Zhang, Chuanming Tan, Xiaoyu Ding, Ning Wang, Xin Liu, Xiaoping Hu, Chun |
author_sort | Feng, Jian |
collection | PubMed |
description | The diaryl ureas are very important fragments in medicinal chemistry. By means of computer-aided design, 1-aryl-3-[4-(pyridin-2-ylmethoxy)phenyl]urea derivatives were designed and synthesized, and evaluated for their antiproliferative activity against A549, HCT-116, PC-3 cancer cell lines, and HL7702 human normal liver cell lines in vitro by using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide colorimetric assay. Most of the target compounds demonstrate significant antiproliferative effects on all the selective cancer cell lines. The calculated IC(50) values were reported. The target compound 1-(4-chlorophenyl)-3-{4-{[3-methyl-4-(2,2,2-trifluoroethoxy)pyridin-2-yl]methoxy}phenyl}urea (7u) demonstrated the most potent inhibitory activity (IC(50) = 2.39 ± 0.10 μM for A549 and IC(50) = 3.90 ± 0.33 μM for HCT-116), comparable to the positive-control sorafenib (IC(50) = 2.12 ± 0.18 μM for A549 and IC(50) = 2.25 ± 0.71 μM for HCT-116). Conclusively, 1-aryl-3-[4-(pyridin-2-ylmethoxy)phenyl]urea derivatives as the new anticancer agents were discovered, and could be used as the potential BRAF inhibitors for further research. |
format | Online Article Text |
id | pubmed-7232929 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2020 |
publisher | Springer US |
record_format | MEDLINE/PubMed |
spelling | pubmed-72329292020-05-18 Synthesis and biological evaluation of a new series of 1-aryl-3-[4-(pyridin-2-ylmethoxy)phenyl]urea derivatives as new anticancer agents Feng, Jian Li, Tai Liang, Shishao Zhang, Chuanming Tan, Xiaoyu Ding, Ning Wang, Xin Liu, Xiaoping Hu, Chun Med Chem Res Original Research The diaryl ureas are very important fragments in medicinal chemistry. By means of computer-aided design, 1-aryl-3-[4-(pyridin-2-ylmethoxy)phenyl]urea derivatives were designed and synthesized, and evaluated for their antiproliferative activity against A549, HCT-116, PC-3 cancer cell lines, and HL7702 human normal liver cell lines in vitro by using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide colorimetric assay. Most of the target compounds demonstrate significant antiproliferative effects on all the selective cancer cell lines. The calculated IC(50) values were reported. The target compound 1-(4-chlorophenyl)-3-{4-{[3-methyl-4-(2,2,2-trifluoroethoxy)pyridin-2-yl]methoxy}phenyl}urea (7u) demonstrated the most potent inhibitory activity (IC(50) = 2.39 ± 0.10 μM for A549 and IC(50) = 3.90 ± 0.33 μM for HCT-116), comparable to the positive-control sorafenib (IC(50) = 2.12 ± 0.18 μM for A549 and IC(50) = 2.25 ± 0.71 μM for HCT-116). Conclusively, 1-aryl-3-[4-(pyridin-2-ylmethoxy)phenyl]urea derivatives as the new anticancer agents were discovered, and could be used as the potential BRAF inhibitors for further research. Springer US 2020-05-18 2020 /pmc/articles/PMC7232929/ /pubmed/32427204 http://dx.doi.org/10.1007/s00044-020-02554-z Text en © Springer Science+Business Media, LLC, part of Springer Nature 2020 This article is made available via the PMC Open Access Subset for unrestricted research re-use and secondary analysis in any form or by any means with acknowledgement of the original source. These permissions are granted for the duration of the World Health Organization (WHO) declaration of COVID-19 as a global pandemic. |
spellingShingle | Original Research Feng, Jian Li, Tai Liang, Shishao Zhang, Chuanming Tan, Xiaoyu Ding, Ning Wang, Xin Liu, Xiaoping Hu, Chun Synthesis and biological evaluation of a new series of 1-aryl-3-[4-(pyridin-2-ylmethoxy)phenyl]urea derivatives as new anticancer agents |
title | Synthesis and biological evaluation of a new series of 1-aryl-3-[4-(pyridin-2-ylmethoxy)phenyl]urea derivatives as new anticancer agents |
title_full | Synthesis and biological evaluation of a new series of 1-aryl-3-[4-(pyridin-2-ylmethoxy)phenyl]urea derivatives as new anticancer agents |
title_fullStr | Synthesis and biological evaluation of a new series of 1-aryl-3-[4-(pyridin-2-ylmethoxy)phenyl]urea derivatives as new anticancer agents |
title_full_unstemmed | Synthesis and biological evaluation of a new series of 1-aryl-3-[4-(pyridin-2-ylmethoxy)phenyl]urea derivatives as new anticancer agents |
title_short | Synthesis and biological evaluation of a new series of 1-aryl-3-[4-(pyridin-2-ylmethoxy)phenyl]urea derivatives as new anticancer agents |
title_sort | synthesis and biological evaluation of a new series of 1-aryl-3-[4-(pyridin-2-ylmethoxy)phenyl]urea derivatives as new anticancer agents |
topic | Original Research |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7232929/ https://www.ncbi.nlm.nih.gov/pubmed/32427204 http://dx.doi.org/10.1007/s00044-020-02554-z |
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