Cargando…

Design, synthesis, antimicrobial and cytotoxicity study on human colorectal carcinoma cell line of new 4,4′-(1,4-phenylene)bis(pyrimidin-2-amine) derivatives

BACKGROUND: Pyrimidine molecules attracted organic chemists very much due to their biological and chemotherapeutic importance. Their related fused heterocycles are of interest as potential bioactive molecules so, we have designed and prepared a new class of 4,4′-(1,4-phenylene)bis(pyrimidin-2-amine)...

Descripción completa

Detalles Bibliográficos
Autores principales: Kumar, Sanjiv, Lim, Siong Meng, Ramasamy, Kalavathy, Mani, Vasudevan, Shah, Syed Adnan Ali, Narasimhan, Balasubramanian
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Springer International Publishing 2018
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6020093/
https://www.ncbi.nlm.nih.gov/pubmed/29938365
http://dx.doi.org/10.1186/s13065-018-0440-3
_version_ 1783335229831774208
author Kumar, Sanjiv
Lim, Siong Meng
Ramasamy, Kalavathy
Mani, Vasudevan
Shah, Syed Adnan Ali
Narasimhan, Balasubramanian
author_facet Kumar, Sanjiv
Lim, Siong Meng
Ramasamy, Kalavathy
Mani, Vasudevan
Shah, Syed Adnan Ali
Narasimhan, Balasubramanian
author_sort Kumar, Sanjiv
collection PubMed
description BACKGROUND: Pyrimidine molecules attracted organic chemists very much due to their biological and chemotherapeutic importance. Their related fused heterocycles are of interest as potential bioactive molecules so, we have designed and prepared a new class of 4,4′-(1,4-phenylene)bis(pyrimidin-2-amine) molecules and screened for their in vitro antibacterial, antifungal and cytotoxicity studies. RESULTS: The structures of synthesized bis-pyrimidine molecules were confirmed by physicochemical and spectral means. The synthesized compounds were further evaluated for their in vitro biological potentials i.e. antimicrobial activity using tube dilution method and anticancer activity against human colorectal carcinoma (HCT116) cancer cell line by Sulforhodamine B assay. CONCLUSIONS: The biological study demonstrated that compounds s7, s8, s11, s14, s16, s17 and s18 have shown more promising antimicrobial activity with best MIC values than the cefadroxil (antibacterial) and fluconazole (antifungal) and compound s3 found to have better anticancer activity against human colorectal carcinoma (HCT116) cancer cell line. [Image: see text]
format Online
Article
Text
id pubmed-6020093
institution National Center for Biotechnology Information
language English
publishDate 2018
publisher Springer International Publishing
record_format MEDLINE/PubMed
spelling pubmed-60200932018-07-13 Design, synthesis, antimicrobial and cytotoxicity study on human colorectal carcinoma cell line of new 4,4′-(1,4-phenylene)bis(pyrimidin-2-amine) derivatives Kumar, Sanjiv Lim, Siong Meng Ramasamy, Kalavathy Mani, Vasudevan Shah, Syed Adnan Ali Narasimhan, Balasubramanian Chem Cent J Research Article BACKGROUND: Pyrimidine molecules attracted organic chemists very much due to their biological and chemotherapeutic importance. Their related fused heterocycles are of interest as potential bioactive molecules so, we have designed and prepared a new class of 4,4′-(1,4-phenylene)bis(pyrimidin-2-amine) molecules and screened for their in vitro antibacterial, antifungal and cytotoxicity studies. RESULTS: The structures of synthesized bis-pyrimidine molecules were confirmed by physicochemical and spectral means. The synthesized compounds were further evaluated for their in vitro biological potentials i.e. antimicrobial activity using tube dilution method and anticancer activity against human colorectal carcinoma (HCT116) cancer cell line by Sulforhodamine B assay. CONCLUSIONS: The biological study demonstrated that compounds s7, s8, s11, s14, s16, s17 and s18 have shown more promising antimicrobial activity with best MIC values than the cefadroxil (antibacterial) and fluconazole (antifungal) and compound s3 found to have better anticancer activity against human colorectal carcinoma (HCT116) cancer cell line. [Image: see text] Springer International Publishing 2018-06-25 /pmc/articles/PMC6020093/ /pubmed/29938365 http://dx.doi.org/10.1186/s13065-018-0440-3 Text en © The Author(s) 2018 Open AccessThis article is distributed under the terms of the Creative Commons Attribution 4.0 International License (http://creativecommons.org/licenses/by/4.0/), which permits unrestricted use, distribution, and reproduction in any medium, provided you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons license, and indicate if changes were made. The Creative Commons Public Domain Dedication waiver (http://creativecommons.org/publicdomain/zero/1.0/) applies to the data made available in this article, unless otherwise stated.
spellingShingle Research Article
Kumar, Sanjiv
Lim, Siong Meng
Ramasamy, Kalavathy
Mani, Vasudevan
Shah, Syed Adnan Ali
Narasimhan, Balasubramanian
Design, synthesis, antimicrobial and cytotoxicity study on human colorectal carcinoma cell line of new 4,4′-(1,4-phenylene)bis(pyrimidin-2-amine) derivatives
title Design, synthesis, antimicrobial and cytotoxicity study on human colorectal carcinoma cell line of new 4,4′-(1,4-phenylene)bis(pyrimidin-2-amine) derivatives
title_full Design, synthesis, antimicrobial and cytotoxicity study on human colorectal carcinoma cell line of new 4,4′-(1,4-phenylene)bis(pyrimidin-2-amine) derivatives
title_fullStr Design, synthesis, antimicrobial and cytotoxicity study on human colorectal carcinoma cell line of new 4,4′-(1,4-phenylene)bis(pyrimidin-2-amine) derivatives
title_full_unstemmed Design, synthesis, antimicrobial and cytotoxicity study on human colorectal carcinoma cell line of new 4,4′-(1,4-phenylene)bis(pyrimidin-2-amine) derivatives
title_short Design, synthesis, antimicrobial and cytotoxicity study on human colorectal carcinoma cell line of new 4,4′-(1,4-phenylene)bis(pyrimidin-2-amine) derivatives
title_sort design, synthesis, antimicrobial and cytotoxicity study on human colorectal carcinoma cell line of new 4,4′-(1,4-phenylene)bis(pyrimidin-2-amine) derivatives
topic Research Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6020093/
https://www.ncbi.nlm.nih.gov/pubmed/29938365
http://dx.doi.org/10.1186/s13065-018-0440-3
work_keys_str_mv AT kumarsanjiv designsynthesisantimicrobialandcytotoxicitystudyonhumancolorectalcarcinomacelllineofnew4414phenylenebispyrimidin2aminederivatives
AT limsiongmeng designsynthesisantimicrobialandcytotoxicitystudyonhumancolorectalcarcinomacelllineofnew4414phenylenebispyrimidin2aminederivatives
AT ramasamykalavathy designsynthesisantimicrobialandcytotoxicitystudyonhumancolorectalcarcinomacelllineofnew4414phenylenebispyrimidin2aminederivatives
AT manivasudevan designsynthesisantimicrobialandcytotoxicitystudyonhumancolorectalcarcinomacelllineofnew4414phenylenebispyrimidin2aminederivatives
AT shahsyedadnanali designsynthesisantimicrobialandcytotoxicitystudyonhumancolorectalcarcinomacelllineofnew4414phenylenebispyrimidin2aminederivatives
AT narasimhanbalasubramanian designsynthesisantimicrobialandcytotoxicitystudyonhumancolorectalcarcinomacelllineofnew4414phenylenebispyrimidin2aminederivatives