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Design, Syntheses, and Bioevaluations of Some Novel N(2)-Acryloylbenzohydrazides as Chemostimulants and Cytotoxic Agents
A series of novel N(2)-acryloylhydrazides 1a–m and a related series of compounds 6a–c were prepared as potential chemostimulants. In general, these compounds are cytotoxic to human HCT 116 colon cancer cells, as well as human MCF-7 and MDA-MB-231 breast cancer cell lines. A representative compound N...
Autores principales: | , , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
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MDPI
2021
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8226474/ https://www.ncbi.nlm.nih.gov/pubmed/34205029 http://dx.doi.org/10.3390/medicines8060027 |
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author | Lakhani, Kinjal Borrego, Edgar A. Cano, Karla G. Dimmock, Jonathan R. Aguilera, Renato J. Das, Swagatika Roayapalley, Praveen K. Sharma, Rajendra K. Das, Umashankar |
author_facet | Lakhani, Kinjal Borrego, Edgar A. Cano, Karla G. Dimmock, Jonathan R. Aguilera, Renato J. Das, Swagatika Roayapalley, Praveen K. Sharma, Rajendra K. Das, Umashankar |
author_sort | Lakhani, Kinjal |
collection | PubMed |
description | A series of novel N(2)-acryloylhydrazides 1a–m and a related series of compounds 6a–c were prepared as potential chemostimulants. In general, these compounds are cytotoxic to human HCT 116 colon cancer cells, as well as human MCF-7 and MDA-MB-231 breast cancer cell lines. A representative compound N(1)-(3,4-dimethoxyphenylcarbonyl)-N(2)-acryloylhydrazine 1m sensitized HCT 116 cells to the potent antineoplastic agent 3,5-bis(benzylidene)-4-piperidone 2a, and also to 5-fluorouracil. A series of compounds was prepared that incorporated some of the molecular features of 2a and related compounds with various N(2)-acryloylhydrazides in series 1. These compounds are potent cytotoxins. Two modes of action of representative compounds are the lowering of mitochondrial membrane potential and increasing the concentration of reactive oxygen species. |
format | Online Article Text |
id | pubmed-8226474 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2021 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-82264742021-06-26 Design, Syntheses, and Bioevaluations of Some Novel N(2)-Acryloylbenzohydrazides as Chemostimulants and Cytotoxic Agents Lakhani, Kinjal Borrego, Edgar A. Cano, Karla G. Dimmock, Jonathan R. Aguilera, Renato J. Das, Swagatika Roayapalley, Praveen K. Sharma, Rajendra K. Das, Umashankar Medicines (Basel) Article A series of novel N(2)-acryloylhydrazides 1a–m and a related series of compounds 6a–c were prepared as potential chemostimulants. In general, these compounds are cytotoxic to human HCT 116 colon cancer cells, as well as human MCF-7 and MDA-MB-231 breast cancer cell lines. A representative compound N(1)-(3,4-dimethoxyphenylcarbonyl)-N(2)-acryloylhydrazine 1m sensitized HCT 116 cells to the potent antineoplastic agent 3,5-bis(benzylidene)-4-piperidone 2a, and also to 5-fluorouracil. A series of compounds was prepared that incorporated some of the molecular features of 2a and related compounds with various N(2)-acryloylhydrazides in series 1. These compounds are potent cytotoxins. Two modes of action of representative compounds are the lowering of mitochondrial membrane potential and increasing the concentration of reactive oxygen species. MDPI 2021-06-03 /pmc/articles/PMC8226474/ /pubmed/34205029 http://dx.doi.org/10.3390/medicines8060027 Text en © 2021 by the authors. https://creativecommons.org/licenses/by/4.0/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 (https://creativecommons.org/licenses/by/4.0/). |
spellingShingle | Article Lakhani, Kinjal Borrego, Edgar A. Cano, Karla G. Dimmock, Jonathan R. Aguilera, Renato J. Das, Swagatika Roayapalley, Praveen K. Sharma, Rajendra K. Das, Umashankar Design, Syntheses, and Bioevaluations of Some Novel N(2)-Acryloylbenzohydrazides as Chemostimulants and Cytotoxic Agents |
title | Design, Syntheses, and Bioevaluations of Some Novel N(2)-Acryloylbenzohydrazides as Chemostimulants and Cytotoxic Agents |
title_full | Design, Syntheses, and Bioevaluations of Some Novel N(2)-Acryloylbenzohydrazides as Chemostimulants and Cytotoxic Agents |
title_fullStr | Design, Syntheses, and Bioevaluations of Some Novel N(2)-Acryloylbenzohydrazides as Chemostimulants and Cytotoxic Agents |
title_full_unstemmed | Design, Syntheses, and Bioevaluations of Some Novel N(2)-Acryloylbenzohydrazides as Chemostimulants and Cytotoxic Agents |
title_short | Design, Syntheses, and Bioevaluations of Some Novel N(2)-Acryloylbenzohydrazides as Chemostimulants and Cytotoxic Agents |
title_sort | design, syntheses, and bioevaluations of some novel n(2)-acryloylbenzohydrazides as chemostimulants and cytotoxic agents |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8226474/ https://www.ncbi.nlm.nih.gov/pubmed/34205029 http://dx.doi.org/10.3390/medicines8060027 |
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