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1H-2,3-Dihydroperimidine Derivatives: A New Class of Potent Protein Tyrosine Phosphatase 1B Inhibitors
A series of 1H-2,3-dihydroperimidine derivatives was designed, synthesized, and evaluated as a new class of inhibitors of protein tyrosine phosphatase 1B (PTP1B) with IC(50) values in the micromolar range. Compounds 46 and 49 showed submicromolar inhibitory activity against PTP1B, and good selectivi...
| Autores principales: | , , , , , , , , , , , , , , , , |
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| Formato: | Online Artículo Texto |
| Lenguaje: | English |
| Publicado: |
MDPI
2013
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| Materias: | |
| Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6271978/ https://www.ncbi.nlm.nih.gov/pubmed/24366088 http://dx.doi.org/10.3390/molecules19010102 |
| _version_ | 1783377053663363072 |
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| author | Wang, Wen-Long Yang, Dong-Lin Gao, Li-Xin Tang, Chun-Lan Ma, Wei-Ping Ye, Hui-Hua Zhang, Si-Qi Zhao, Ya-Nan Xu, Hao-Jie Hu, Zhao Chen, Xia Fan, Wen-Hua Chen, Hai-Jun Li, Jing-Ya Nan, Fa-Jun Li, Jia Feng, Bainian |
| author_facet | Wang, Wen-Long Yang, Dong-Lin Gao, Li-Xin Tang, Chun-Lan Ma, Wei-Ping Ye, Hui-Hua Zhang, Si-Qi Zhao, Ya-Nan Xu, Hao-Jie Hu, Zhao Chen, Xia Fan, Wen-Hua Chen, Hai-Jun Li, Jing-Ya Nan, Fa-Jun Li, Jia Feng, Bainian |
| author_sort | Wang, Wen-Long |
| collection | PubMed |
| description | A series of 1H-2,3-dihydroperimidine derivatives was designed, synthesized, and evaluated as a new class of inhibitors of protein tyrosine phosphatase 1B (PTP1B) with IC(50) values in the micromolar range. Compounds 46 and 49 showed submicromolar inhibitory activity against PTP1B, and good selectivity (3.48-fold and 2.10-fold respectively) over T-cell protein tyrosine phosphatases (TCPTP). These results have provided novel lead compounds for the design of inhibitors of PTP1B as well as other PTPs. |
| format | Online Article Text |
| id | pubmed-6271978 |
| institution | National Center for Biotechnology Information |
| language | English |
| publishDate | 2013 |
| publisher | MDPI |
| record_format | MEDLINE/PubMed |
| spelling | pubmed-62719782018-12-20 1H-2,3-Dihydroperimidine Derivatives: A New Class of Potent Protein Tyrosine Phosphatase 1B Inhibitors Wang, Wen-Long Yang, Dong-Lin Gao, Li-Xin Tang, Chun-Lan Ma, Wei-Ping Ye, Hui-Hua Zhang, Si-Qi Zhao, Ya-Nan Xu, Hao-Jie Hu, Zhao Chen, Xia Fan, Wen-Hua Chen, Hai-Jun Li, Jing-Ya Nan, Fa-Jun Li, Jia Feng, Bainian Molecules Article A series of 1H-2,3-dihydroperimidine derivatives was designed, synthesized, and evaluated as a new class of inhibitors of protein tyrosine phosphatase 1B (PTP1B) with IC(50) values in the micromolar range. Compounds 46 and 49 showed submicromolar inhibitory activity against PTP1B, and good selectivity (3.48-fold and 2.10-fold respectively) over T-cell protein tyrosine phosphatases (TCPTP). These results have provided novel lead compounds for the design of inhibitors of PTP1B as well as other PTPs. MDPI 2013-12-23 /pmc/articles/PMC6271978/ /pubmed/24366088 http://dx.doi.org/10.3390/molecules19010102 Text en © 2013 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution license (http://creativecommons.org/licenses/by/3.0/). |
| spellingShingle | Article Wang, Wen-Long Yang, Dong-Lin Gao, Li-Xin Tang, Chun-Lan Ma, Wei-Ping Ye, Hui-Hua Zhang, Si-Qi Zhao, Ya-Nan Xu, Hao-Jie Hu, Zhao Chen, Xia Fan, Wen-Hua Chen, Hai-Jun Li, Jing-Ya Nan, Fa-Jun Li, Jia Feng, Bainian 1H-2,3-Dihydroperimidine Derivatives: A New Class of Potent Protein Tyrosine Phosphatase 1B Inhibitors |
| title | 1H-2,3-Dihydroperimidine Derivatives: A New Class of Potent Protein Tyrosine Phosphatase 1B Inhibitors |
| title_full | 1H-2,3-Dihydroperimidine Derivatives: A New Class of Potent Protein Tyrosine Phosphatase 1B Inhibitors |
| title_fullStr | 1H-2,3-Dihydroperimidine Derivatives: A New Class of Potent Protein Tyrosine Phosphatase 1B Inhibitors |
| title_full_unstemmed | 1H-2,3-Dihydroperimidine Derivatives: A New Class of Potent Protein Tyrosine Phosphatase 1B Inhibitors |
| title_short | 1H-2,3-Dihydroperimidine Derivatives: A New Class of Potent Protein Tyrosine Phosphatase 1B Inhibitors |
| title_sort | 1h-2,3-dihydroperimidine derivatives: a new class of potent protein tyrosine phosphatase 1b inhibitors |
| topic | Article |
| url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6271978/ https://www.ncbi.nlm.nih.gov/pubmed/24366088 http://dx.doi.org/10.3390/molecules19010102 |
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