Cargando…

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...

Descripción completa

Detalles Bibliográficos
Autores principales: Ding, Ying, Zhao, Lianbo, Fu, Ying, Hao, Lei, Fu, Yupeng, Yuan, Yuan, Yu, Peng, Teng, Yuou
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2020
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
_version_ 1783634502913884160
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
work_keys_str_mv AT dingying synthesisandantiproliferatoryactivitiesevaluationofmultisubstitutedisatinderivatives
AT zhaolianbo synthesisandantiproliferatoryactivitiesevaluationofmultisubstitutedisatinderivatives
AT fuying synthesisandantiproliferatoryactivitiesevaluationofmultisubstitutedisatinderivatives
AT haolei synthesisandantiproliferatoryactivitiesevaluationofmultisubstitutedisatinderivatives
AT fuyupeng synthesisandantiproliferatoryactivitiesevaluationofmultisubstitutedisatinderivatives
AT yuanyuan synthesisandantiproliferatoryactivitiesevaluationofmultisubstitutedisatinderivatives
AT yupeng synthesisandantiproliferatoryactivitiesevaluationofmultisubstitutedisatinderivatives
AT tengyuou synthesisandantiproliferatoryactivitiesevaluationofmultisubstitutedisatinderivatives