Design, Synthesis, and Anticancer Activities of Novel 2-Amino-4-phenylthiazole Scaffold Containing Amide Moieties
Appropriately substituted 2-amino-4-phenylthiazole derivatives were designed and synthesized according to the structural characteristics of crizotinib. The obtained compounds were characterized using 1H NMR, 13C NMR, and HRMS. The target compounds 5a–o were evaluated for their in vitro antiprolifera...
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| Main Authors: | , , , , , , , , |
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| Format: | Article |
| Language: | English |
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Wiley
2018-01-01
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| Series: | Journal of Chemistry |
| Online Access: | http://dx.doi.org/10.1155/2018/4301910 |
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| author | Zhi-Hua Zhang Hong-Mei Wu Sai-Nan Deng Xiao-Yu Cai Yu Yao Muriira Cyrus Mwenda Jin-Yin Wang Dong Cai Yu Chen |
| author_facet | Zhi-Hua Zhang Hong-Mei Wu Sai-Nan Deng Xiao-Yu Cai Yu Yao Muriira Cyrus Mwenda Jin-Yin Wang Dong Cai Yu Chen |
| author_sort | Zhi-Hua Zhang |
| collection | DOAJ |
| description | Appropriately substituted 2-amino-4-phenylthiazole derivatives were designed and synthesized according to the structural characteristics of crizotinib. The obtained compounds were characterized using 1H NMR, 13C NMR, and HRMS. The target compounds 5a–o were evaluated for their in vitro antiproliferative activity against A549, HeLa, HT29, and Karpas299 human cancer cell lines. Based on results of biological studies, some of these compounds exhibited significant antiproliferative activity. Compound 5b possessed outstanding growth inhibitory effects on the four cell lines, especially for HT29 cell with IC50 value of 2.01 µM. Along with the biological assay data, a molecular docking study suggests that the target compounds were a potential inhibitor. |
| format | Article |
| id | doaj-art-2aab7a7dd0114aadad7b9ceb56f8e7eb |
| institution | Kabale University |
| issn | 2090-9063 2090-9071 |
| language | English |
| publishDate | 2018-01-01 |
| publisher | Wiley |
| record_format | Article |
| series | Journal of Chemistry |
| spelling | doaj-art-2aab7a7dd0114aadad7b9ceb56f8e7eb2025-08-20T03:54:42ZengWileyJournal of Chemistry2090-90632090-90712018-01-01201810.1155/2018/43019104301910Design, Synthesis, and Anticancer Activities of Novel 2-Amino-4-phenylthiazole Scaffold Containing Amide MoietiesZhi-Hua Zhang0Hong-Mei Wu1Sai-Nan Deng2Xiao-Yu Cai3Yu Yao4Muriira Cyrus Mwenda5Jin-Yin Wang6Dong Cai7Yu Chen8School of Chemical and Environmental Engineering, Liaoning University of Technology, Jinzhou 121001, ChinaSchool of Chemical and Environmental Engineering, Liaoning University of Technology, Jinzhou 121001, ChinaCollege of Pharmacy, Jinzhou Medical University, Jinzhou 121001, ChinaCollege of Pharmacy, Jinzhou Medical University, Jinzhou 121001, ChinaCollege of Pharmacy, Jinzhou Medical University, Jinzhou 121001, ChinaCollege of Pharmacy, Jinzhou Medical University, Jinzhou 121001, ChinaCollege of Pharmacy, Jinzhou Medical University, Jinzhou 121001, ChinaCollege of Public Basic Sciences, Jinzhou Medical University, Jinzhou 121001, ChinaSchool of Chemical and Environmental Engineering, Liaoning University of Technology, Jinzhou 121001, ChinaAppropriately substituted 2-amino-4-phenylthiazole derivatives were designed and synthesized according to the structural characteristics of crizotinib. The obtained compounds were characterized using 1H NMR, 13C NMR, and HRMS. The target compounds 5a–o were evaluated for their in vitro antiproliferative activity against A549, HeLa, HT29, and Karpas299 human cancer cell lines. Based on results of biological studies, some of these compounds exhibited significant antiproliferative activity. Compound 5b possessed outstanding growth inhibitory effects on the four cell lines, especially for HT29 cell with IC50 value of 2.01 µM. Along with the biological assay data, a molecular docking study suggests that the target compounds were a potential inhibitor.http://dx.doi.org/10.1155/2018/4301910 |
| spellingShingle | Zhi-Hua Zhang Hong-Mei Wu Sai-Nan Deng Xiao-Yu Cai Yu Yao Muriira Cyrus Mwenda Jin-Yin Wang Dong Cai Yu Chen Design, Synthesis, and Anticancer Activities of Novel 2-Amino-4-phenylthiazole Scaffold Containing Amide Moieties Journal of Chemistry |
| title | Design, Synthesis, and Anticancer Activities of Novel 2-Amino-4-phenylthiazole Scaffold Containing Amide Moieties |
| title_full | Design, Synthesis, and Anticancer Activities of Novel 2-Amino-4-phenylthiazole Scaffold Containing Amide Moieties |
| title_fullStr | Design, Synthesis, and Anticancer Activities of Novel 2-Amino-4-phenylthiazole Scaffold Containing Amide Moieties |
| title_full_unstemmed | Design, Synthesis, and Anticancer Activities of Novel 2-Amino-4-phenylthiazole Scaffold Containing Amide Moieties |
| title_short | Design, Synthesis, and Anticancer Activities of Novel 2-Amino-4-phenylthiazole Scaffold Containing Amide Moieties |
| title_sort | design synthesis and anticancer activities of novel 2 amino 4 phenylthiazole scaffold containing amide moieties |
| url | http://dx.doi.org/10.1155/2018/4301910 |
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