Cargando…

Synthesis, X-ray Analysis, Biological Evaluation and Molecular Docking Study of New Thiazoline Derivatives

A series of new thiazoline derivatives were synthesized. Structure analyses were accomplished employing (1)H-NMR, (13)C-NMR, X-ray and MS techniques. The in vitro antitumor activities were assessed against human hepatocellular carcinoma (HepG-2) and colorectal carcinoma (HCT-116) cell lines. The res...

Descripción completa

Detalles Bibliográficos
Autores principales: Mabkhot, Yahia N., Algarni, H., Alsayari, Abdulrhman, Bin Muhsinah, Abdullatif, Kheder, Nabila A., Almarhoon, Zainab M., Al-aizari, Faiz A.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2019
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6540005/
https://www.ncbi.nlm.nih.gov/pubmed/31035531
http://dx.doi.org/10.3390/molecules24091654
_version_ 1783422523339177984
author Mabkhot, Yahia N.
Algarni, H.
Alsayari, Abdulrhman
Bin Muhsinah, Abdullatif
Kheder, Nabila A.
Almarhoon, Zainab M.
Al-aizari, Faiz A.
author_facet Mabkhot, Yahia N.
Algarni, H.
Alsayari, Abdulrhman
Bin Muhsinah, Abdullatif
Kheder, Nabila A.
Almarhoon, Zainab M.
Al-aizari, Faiz A.
author_sort Mabkhot, Yahia N.
collection PubMed
description A series of new thiazoline derivatives were synthesized. Structure analyses were accomplished employing (1)H-NMR, (13)C-NMR, X-ray and MS techniques. The in vitro antitumor activities were assessed against human hepatocellular carcinoma (HepG-2) and colorectal carcinoma (HCT-116) cell lines. The results revealed that the thiazolines 5b and 2c exhibited significant activity against the two cell lines. The in vitro antimicrobial screening showed that the thiazolines 2c, 5b and 5d showed promising inhibition activity against Salmonella sp. Additionally, the inhibition activity of thiazolines 2e and 5b against Escherichia coli was comparable to that of the reference compound gentamycin.
format Online
Article
Text
id pubmed-6540005
institution National Center for Biotechnology Information
language English
publishDate 2019
publisher MDPI
record_format MEDLINE/PubMed
spelling pubmed-65400052019-05-31 Synthesis, X-ray Analysis, Biological Evaluation and Molecular Docking Study of New Thiazoline Derivatives Mabkhot, Yahia N. Algarni, H. Alsayari, Abdulrhman Bin Muhsinah, Abdullatif Kheder, Nabila A. Almarhoon, Zainab M. Al-aizari, Faiz A. Molecules Article A series of new thiazoline derivatives were synthesized. Structure analyses were accomplished employing (1)H-NMR, (13)C-NMR, X-ray and MS techniques. The in vitro antitumor activities were assessed against human hepatocellular carcinoma (HepG-2) and colorectal carcinoma (HCT-116) cell lines. The results revealed that the thiazolines 5b and 2c exhibited significant activity against the two cell lines. The in vitro antimicrobial screening showed that the thiazolines 2c, 5b and 5d showed promising inhibition activity against Salmonella sp. Additionally, the inhibition activity of thiazolines 2e and 5b against Escherichia coli was comparable to that of the reference compound gentamycin. MDPI 2019-04-26 /pmc/articles/PMC6540005/ /pubmed/31035531 http://dx.doi.org/10.3390/molecules24091654 Text en © 2019 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
Mabkhot, Yahia N.
Algarni, H.
Alsayari, Abdulrhman
Bin Muhsinah, Abdullatif
Kheder, Nabila A.
Almarhoon, Zainab M.
Al-aizari, Faiz A.
Synthesis, X-ray Analysis, Biological Evaluation and Molecular Docking Study of New Thiazoline Derivatives
title Synthesis, X-ray Analysis, Biological Evaluation and Molecular Docking Study of New Thiazoline Derivatives
title_full Synthesis, X-ray Analysis, Biological Evaluation and Molecular Docking Study of New Thiazoline Derivatives
title_fullStr Synthesis, X-ray Analysis, Biological Evaluation and Molecular Docking Study of New Thiazoline Derivatives
title_full_unstemmed Synthesis, X-ray Analysis, Biological Evaluation and Molecular Docking Study of New Thiazoline Derivatives
title_short Synthesis, X-ray Analysis, Biological Evaluation and Molecular Docking Study of New Thiazoline Derivatives
title_sort synthesis, x-ray analysis, biological evaluation and molecular docking study of new thiazoline derivatives
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6540005/
https://www.ncbi.nlm.nih.gov/pubmed/31035531
http://dx.doi.org/10.3390/molecules24091654
work_keys_str_mv AT mabkhotyahian synthesisxrayanalysisbiologicalevaluationandmoleculardockingstudyofnewthiazolinederivatives
AT algarnih synthesisxrayanalysisbiologicalevaluationandmoleculardockingstudyofnewthiazolinederivatives
AT alsayariabdulrhman synthesisxrayanalysisbiologicalevaluationandmoleculardockingstudyofnewthiazolinederivatives
AT binmuhsinahabdullatif synthesisxrayanalysisbiologicalevaluationandmoleculardockingstudyofnewthiazolinederivatives
AT khedernabilaa synthesisxrayanalysisbiologicalevaluationandmoleculardockingstudyofnewthiazolinederivatives
AT almarhoonzainabm synthesisxrayanalysisbiologicalevaluationandmoleculardockingstudyofnewthiazolinederivatives
AT alaizarifaiza synthesisxrayanalysisbiologicalevaluationandmoleculardockingstudyofnewthiazolinederivatives