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
2021-12-01
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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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doaj-08397027d6ee4fc0ad27897cbb6ada7f2021-01-01T00:06:33ZengMDPI AGMolecules1420-30492021-12-012617617610.3390/molecules26010176Synthesis and Antiproliferatory Activities Evaluation of Multi-Substituted Isatin DerivativesYing DingLianbo Zhao0Ying Fu1Lei Hao2Yupeng Fu3Yuan Yuan4Peng Yu5Yuou Teng6China 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 |
| collection |
DOAJ |
| language |
English |
| format |
Article |
| sources |
DOAJ |
| author |
Ying Ding Lianbo Zhao Ying Fu Lei Hao Yupeng Fu Yuan Yuan Peng Yu Yuou Teng |
| 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 |
| author_facet |
Ying Ding Lianbo Zhao Ying Fu Lei Hao Yupeng Fu Yuan Yuan Peng Yu Yuou Teng |
| author_sort |
Ying Ding |
| title |
Synthesis and Antiproliferatory Activities Evaluation of Multi-Substituted Isatin Derivatives |
| title_short |
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_sort |
synthesis and antiproliferatory activities evaluation of multi-substituted isatin derivatives |
| publisher |
MDPI AG |
| series |
Molecules |
| issn |
1420-3049 |
| publishDate |
2021-12-01 |
| 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. |
| 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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