N-Propargylated isatin-Mannich mono- and bis-adducts: Synthesis and preliminary analysis of in vitro activity against Tritrichomonas foetus

Cu(I)Cl promoted synthesis of N-propargylated-isatin Mannich mono- and bis-adducts with an extension towards the synthesis of N-propargylated-isatin-7-chloroquinoline conjugates was described. The synthesized scaffolds were evaluated for their in vitro activity against the veterinary protozoal patho...

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Autores principales: Nisha, Kumar, Kewal, Bhargava, Gaurav, Land, Kirkwood M., Chang, Kai-Hsiang, Arora, Reena, Sen, Somdutta, Kumar, Vipan
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Elsevier Masson SAS. 2014
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7115568/
https://www.ncbi.nlm.nih.gov/pubmed/24561663
http://dx.doi.org/10.1016/j.ejmech.2014.01.015
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author Nisha
Kumar, Kewal
Bhargava, Gaurav
Land, Kirkwood M.
Chang, Kai-Hsiang
Arora, Reena
Sen, Somdutta
Kumar, Vipan
author_facet Nisha
Kumar, Kewal
Bhargava, Gaurav
Land, Kirkwood M.
Chang, Kai-Hsiang
Arora, Reena
Sen, Somdutta
Kumar, Vipan
author_sort Nisha
collection PubMed
description Cu(I)Cl promoted synthesis of N-propargylated-isatin Mannich mono- and bis-adducts with an extension towards the synthesis of N-propargylated-isatin-7-chloroquinoline conjugates was described. The synthesized scaffolds were evaluated for their in vitro activity against the veterinary protozoal pathogen Tritrichomonas foetus and cytotoxicity against human prostate (PC-3) cancer cell line. The preliminary evaluation data revealed the enhancement in the activity profiles with the introduction of 7-chloroquinoline ring with the most active conjugates 7a, 7c and 7d exhibiting an IC(50) of 22.2, 11.3 and 24.5 μM respectively against T. foetus and minimal toxicity against human prostate (PC-3) cell lines.
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spelling pubmed-71155682020-04-02 N-Propargylated isatin-Mannich mono- and bis-adducts: Synthesis and preliminary analysis of in vitro activity against Tritrichomonas foetus Nisha Kumar, Kewal Bhargava, Gaurav Land, Kirkwood M. Chang, Kai-Hsiang Arora, Reena Sen, Somdutta Kumar, Vipan Eur J Med Chem Article Cu(I)Cl promoted synthesis of N-propargylated-isatin Mannich mono- and bis-adducts with an extension towards the synthesis of N-propargylated-isatin-7-chloroquinoline conjugates was described. The synthesized scaffolds were evaluated for their in vitro activity against the veterinary protozoal pathogen Tritrichomonas foetus and cytotoxicity against human prostate (PC-3) cancer cell line. The preliminary evaluation data revealed the enhancement in the activity profiles with the introduction of 7-chloroquinoline ring with the most active conjugates 7a, 7c and 7d exhibiting an IC(50) of 22.2, 11.3 and 24.5 μM respectively against T. foetus and minimal toxicity against human prostate (PC-3) cell lines. Elsevier Masson SAS. 2014-03-03 2014-01-17 /pmc/articles/PMC7115568/ /pubmed/24561663 http://dx.doi.org/10.1016/j.ejmech.2014.01.015 Text en Copyright © 2014 Elsevier Masson SAS. All rights reserved. Since January 2020 Elsevier has created a COVID-19 resource centre with free information in English and Mandarin on the novel coronavirus COVID-19. The COVID-19 resource centre is hosted on Elsevier Connect, the company's public news and information website. Elsevier hereby grants permission to make all its COVID-19-related research that is available on the COVID-19 resource centre - including this research content - immediately available in PubMed Central and other publicly funded repositories, such as the WHO COVID database with rights for unrestricted research re-use and analyses in any form or by any means with acknowledgement of the original source. These permissions are granted for free by Elsevier for as long as the COVID-19 resource centre remains active.
spellingShingle Article
Nisha
Kumar, Kewal
Bhargava, Gaurav
Land, Kirkwood M.
Chang, Kai-Hsiang
Arora, Reena
Sen, Somdutta
Kumar, Vipan
N-Propargylated isatin-Mannich mono- and bis-adducts: Synthesis and preliminary analysis of in vitro activity against Tritrichomonas foetus
title N-Propargylated isatin-Mannich mono- and bis-adducts: Synthesis and preliminary analysis of in vitro activity against Tritrichomonas foetus
title_full N-Propargylated isatin-Mannich mono- and bis-adducts: Synthesis and preliminary analysis of in vitro activity against Tritrichomonas foetus
title_fullStr N-Propargylated isatin-Mannich mono- and bis-adducts: Synthesis and preliminary analysis of in vitro activity against Tritrichomonas foetus
title_full_unstemmed N-Propargylated isatin-Mannich mono- and bis-adducts: Synthesis and preliminary analysis of in vitro activity against Tritrichomonas foetus
title_short N-Propargylated isatin-Mannich mono- and bis-adducts: Synthesis and preliminary analysis of in vitro activity against Tritrichomonas foetus
title_sort n-propargylated isatin-mannich mono- and bis-adducts: synthesis and preliminary analysis of in vitro activity against tritrichomonas foetus
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7115568/
https://www.ncbi.nlm.nih.gov/pubmed/24561663
http://dx.doi.org/10.1016/j.ejmech.2014.01.015
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