Synthesis and Antiproliferatory Activities Evaluation of Multi-Substituted Isatin Derivatives
A series of multi-substituted isatin derivatives were synthesized using the powerful Sandmeyer reaction. The structures of these derivatives were confirmed by <sup>1</sup>H-NMR, <sup>13</sup>C-NMR, and HR-MS. Inhibition of proliferation activities of these derivatives against...
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MDPI AG
2020-12-01
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| Series: | Molecules |
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| Online Access: | https://www.mdpi.com/1420-3049/26/1/176 |
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| author | Ying Ding Lianbo Zhao Ying Fu Lei Hao Yupeng Fu Yuan Yuan Peng Yu Yuou Teng |
| author_facet | Ying Ding Lianbo Zhao Ying Fu Lei Hao Yupeng Fu Yuan Yuan Peng Yu Yuou Teng |
| author_sort | Ying Ding |
| collection | DOAJ |
| description | A series of multi-substituted isatin derivatives were synthesized using the powerful Sandmeyer reaction. The structures of these derivatives were confirmed by <sup>1</sup>H-NMR, <sup>13</sup>C-NMR, and HR-MS. Inhibition of proliferation activities of these derivatives against human leukemia cells (K562), human hepatocellular carcinoma cells (HepG2) and human colon carcinoma cells (HT-29) were evaluated in vitro using the MTT assay. Among the series, compound <b>4l</b> exhibited strong antiproliferatory activities against K562, HepG2 and HT-29 cells with IC<sub>50</sub> values of 1.75, 3.20, and 4.17 μM, respectively. The morphological, growth inhibitory and apoptosic effects of compound <b>4l</b> in K562 cells, wound healing effect in HepG2 cells, and tube formating effect in matrix gel of HUVEC cells were evaluated consequently. All results indicated that compound <b>4l</b> could be used as a potential antitumor agent in further investigations. |
| first_indexed | 2024-03-10T13:34:30Z |
| format | Article |
| id | doaj.art-08397027d6ee4fc0ad27897cbb6ada7f |
| institution | Directory Open Access Journal |
| issn | 1420-3049 |
| language | English |
| last_indexed | 2024-03-10T13:34:30Z |
| publishDate | 2020-12-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Molecules |
| spelling | doaj.art-08397027d6ee4fc0ad27897cbb6ada7f2023-11-21T07:38:00ZengMDPI AGMolecules1420-30492020-12-0126117610.3390/molecules26010176Synthesis and Antiproliferatory Activities Evaluation of Multi-Substituted Isatin DerivativesYing Ding0Lianbo Zhao1Ying Fu2Lei Hao3Yupeng Fu4Yuan Yuan5Peng Yu6Yuou Teng7China International Science and Technology Cooperation Base of Food Nutrition/Safety and Medicinal Chemistry, College of Bioengineering, Tianjin University of Science and Technology, Tianjin 300457, ChinaChina International Science and Technology Cooperation Base of Food Nutrition/Safety and Medicinal Chemistry, College of Bioengineering, Tianjin University of Science and Technology, Tianjin 300457, ChinaChina International Science and Technology Cooperation Base of Food Nutrition/Safety and Medicinal Chemistry, College of Bioengineering, Tianjin University of Science and Technology, Tianjin 300457, ChinaChina International Science and Technology Cooperation Base of Food Nutrition/Safety and Medicinal Chemistry, College of Bioengineering, Tianjin University of Science and Technology, Tianjin 300457, ChinaChina International Science and Technology Cooperation Base of Food Nutrition/Safety and Medicinal Chemistry, College of Bioengineering, Tianjin University of Science and Technology, Tianjin 300457, ChinaChina International Science and Technology Cooperation Base of Food Nutrition/Safety and Medicinal Chemistry, College of Bioengineering, Tianjin University of Science and Technology, Tianjin 300457, ChinaChina International Science and Technology Cooperation Base of Food Nutrition/Safety and Medicinal Chemistry, College of Bioengineering, Tianjin University of Science and Technology, Tianjin 300457, ChinaChina International Science and Technology Cooperation Base of Food Nutrition/Safety and Medicinal Chemistry, College of Bioengineering, Tianjin University of Science and Technology, Tianjin 300457, ChinaA series of multi-substituted isatin derivatives were synthesized using the powerful Sandmeyer reaction. The structures of these derivatives were confirmed by <sup>1</sup>H-NMR, <sup>13</sup>C-NMR, and HR-MS. Inhibition of proliferation activities of these derivatives against human leukemia cells (K562), human hepatocellular carcinoma cells (HepG2) and human colon carcinoma cells (HT-29) were evaluated in vitro using the MTT assay. Among the series, compound <b>4l</b> exhibited strong antiproliferatory activities against K562, HepG2 and HT-29 cells with IC<sub>50</sub> values of 1.75, 3.20, and 4.17 μM, respectively. The morphological, growth inhibitory and apoptosic effects of compound <b>4l</b> in K562 cells, wound healing effect in HepG2 cells, and tube formating effect in matrix gel of HUVEC cells were evaluated consequently. All results indicated that compound <b>4l</b> could be used as a potential antitumor agent in further investigations.https://www.mdpi.com/1420-3049/26/1/176Sandmeyer reactionmulti-substituted isatin derivativescytotoxicitiesapoptosismigrationtube formation |
| spellingShingle | Ying Ding Lianbo Zhao Ying Fu Lei Hao Yupeng Fu Yuan Yuan Peng Yu Yuou Teng Synthesis and Antiproliferatory Activities Evaluation of Multi-Substituted Isatin Derivatives Molecules Sandmeyer reaction multi-substituted isatin derivatives cytotoxicities apoptosis migration tube formation |
| title | Synthesis and Antiproliferatory Activities Evaluation of Multi-Substituted Isatin Derivatives |
| title_full | Synthesis and Antiproliferatory Activities Evaluation of Multi-Substituted Isatin Derivatives |
| title_fullStr | Synthesis and Antiproliferatory Activities Evaluation of Multi-Substituted Isatin Derivatives |
| title_full_unstemmed | Synthesis and Antiproliferatory Activities Evaluation of Multi-Substituted Isatin Derivatives |
| title_short | Synthesis and Antiproliferatory Activities Evaluation of Multi-Substituted Isatin Derivatives |
| title_sort | synthesis and antiproliferatory activities evaluation of multi substituted isatin derivatives |
| topic | Sandmeyer reaction multi-substituted isatin derivatives cytotoxicities apoptosis migration tube formation |
| url | https://www.mdpi.com/1420-3049/26/1/176 |
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