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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 (1)H-NMR, (13)C-NMR, and HR-MS. Inhibition of proliferation activities of these derivatives against human leukemia cells (K562), human hepato...
Autores principales: | , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2020
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7795683/ https://www.ncbi.nlm.nih.gov/pubmed/33396550 http://dx.doi.org/10.3390/molecules26010176 |
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author | Ding, Ying Zhao, Lianbo Fu, Ying Hao, Lei Fu, Yupeng Yuan, Yuan Yu, Peng Teng, Yuou |
author_facet | Ding, Ying Zhao, Lianbo Fu, Ying Hao, Lei Fu, Yupeng Yuan, Yuan Yu, Peng Teng, Yuou |
author_sort | Ding, Ying |
collection | PubMed |
description | A series of multi-substituted isatin derivatives were synthesized using the powerful Sandmeyer reaction. The structures of these derivatives were confirmed by (1)H-NMR, (13)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 4l exhibited strong antiproliferatory activities against K562, HepG2 and HT-29 cells with IC(50) values of 1.75, 3.20, and 4.17 μM, respectively. The morphological, growth inhibitory and apoptosic effects of compound 4l 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 4l could be used as a potential antitumor agent in further investigations. |
format | Online Article Text |
id | pubmed-7795683 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2020 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-77956832021-01-10 Synthesis and Antiproliferatory Activities Evaluation of Multi-Substituted Isatin Derivatives Ding, Ying Zhao, Lianbo Fu, Ying Hao, Lei Fu, Yupeng Yuan, Yuan Yu, Peng Teng, Yuou Molecules Article A series of multi-substituted isatin derivatives were synthesized using the powerful Sandmeyer reaction. The structures of these derivatives were confirmed by (1)H-NMR, (13)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 4l exhibited strong antiproliferatory activities against K562, HepG2 and HT-29 cells with IC(50) values of 1.75, 3.20, and 4.17 μM, respectively. The morphological, growth inhibitory and apoptosic effects of compound 4l 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 4l could be used as a potential antitumor agent in further investigations. MDPI 2020-12-31 /pmc/articles/PMC7795683/ /pubmed/33396550 http://dx.doi.org/10.3390/molecules26010176 Text en © 2020 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 (CC BY) license (http://creativecommons.org/licenses/by/4.0/). |
spellingShingle | Article Ding, Ying Zhao, Lianbo Fu, Ying Hao, Lei Fu, Yupeng Yuan, Yuan Yu, Peng Teng, Yuou Synthesis and Antiproliferatory Activities Evaluation of Multi-Substituted Isatin Derivatives |
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 | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7795683/ https://www.ncbi.nlm.nih.gov/pubmed/33396550 http://dx.doi.org/10.3390/molecules26010176 |
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