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Antiproliferative Activity of New Pyrazole-4-sulfonamide Derivatives: Synthesis and Biological Evaluation
[Image: see text] Pyrazole and sulfonamide constitute an important class of drugs, with several types of pharmacological agents. Facile synthesis of two new series of 3,5-dimethyl-1H-pyrazole-4-sulfonamide and 1,3,5-trimethyl-1H-pyrazole-4-sulfonamide derivatives was designed and synthesized. These...
Autores principales: | , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
American Chemical Society
2023
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Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10373183/ https://www.ncbi.nlm.nih.gov/pubmed/37521676 http://dx.doi.org/10.1021/acsomega.2c07539 |
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author | Mahesh, Panasa Akshinthala, Parameswari Katari, Naresh Kumar Gupta, Lavleen Kumar Panwar, Dikshita Sharma, Manoj Kumar Jonnalagadda, Sreekantha Babu Gundla, Rambabu |
author_facet | Mahesh, Panasa Akshinthala, Parameswari Katari, Naresh Kumar Gupta, Lavleen Kumar Panwar, Dikshita Sharma, Manoj Kumar Jonnalagadda, Sreekantha Babu Gundla, Rambabu |
author_sort | Mahesh, Panasa |
collection | PubMed |
description | [Image: see text] Pyrazole and sulfonamide constitute an important class of drugs, with several types of pharmacological agents. Facile synthesis of two new series of 3,5-dimethyl-1H-pyrazole-4-sulfonamide and 1,3,5-trimethyl-1H-pyrazole-4-sulfonamide derivatives was designed and synthesized. These pyrazole-4-sulfonamide derivatives are characterized by Fourier transform infrared (FT-IR), (1)H NMR, (13)C NMR, and elemental analysis, and their biological evolution data are presented. This paved way for the development of new pyrazole-4-sulfonamide derivatives. These compounds are tested for their in vitro antiproliferative activity against U937 cells by the CellTiter-Glo Luminescent cell viability assay using Mitomycin C. Cytotoxicity detection is based on the measurement of LDH activity, while these compounds did not exhibit cytotoxic activity on these cells. Half maximal inhibitory concentration (IC(50)) was calculated by Graph Pad Prism software for each dose. Their structure–activity relationships were obtained and discussed. |
format | Online Article Text |
id | pubmed-10373183 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2023 |
publisher | American Chemical Society |
record_format | MEDLINE/PubMed |
spelling | pubmed-103731832023-07-28 Antiproliferative Activity of New Pyrazole-4-sulfonamide Derivatives: Synthesis and Biological Evaluation Mahesh, Panasa Akshinthala, Parameswari Katari, Naresh Kumar Gupta, Lavleen Kumar Panwar, Dikshita Sharma, Manoj Kumar Jonnalagadda, Sreekantha Babu Gundla, Rambabu ACS Omega [Image: see text] Pyrazole and sulfonamide constitute an important class of drugs, with several types of pharmacological agents. Facile synthesis of two new series of 3,5-dimethyl-1H-pyrazole-4-sulfonamide and 1,3,5-trimethyl-1H-pyrazole-4-sulfonamide derivatives was designed and synthesized. These pyrazole-4-sulfonamide derivatives are characterized by Fourier transform infrared (FT-IR), (1)H NMR, (13)C NMR, and elemental analysis, and their biological evolution data are presented. This paved way for the development of new pyrazole-4-sulfonamide derivatives. These compounds are tested for their in vitro antiproliferative activity against U937 cells by the CellTiter-Glo Luminescent cell viability assay using Mitomycin C. Cytotoxicity detection is based on the measurement of LDH activity, while these compounds did not exhibit cytotoxic activity on these cells. Half maximal inhibitory concentration (IC(50)) was calculated by Graph Pad Prism software for each dose. Their structure–activity relationships were obtained and discussed. American Chemical Society 2023-07-13 /pmc/articles/PMC10373183/ /pubmed/37521676 http://dx.doi.org/10.1021/acsomega.2c07539 Text en © 2023 The Authors. Published by American Chemical Society https://creativecommons.org/licenses/by-nc-nd/4.0/Permits non-commercial access and re-use, provided that author attribution and integrity are maintained; but does not permit creation of adaptations or other derivative works (https://creativecommons.org/licenses/by-nc-nd/4.0/). |
spellingShingle | Mahesh, Panasa Akshinthala, Parameswari Katari, Naresh Kumar Gupta, Lavleen Kumar Panwar, Dikshita Sharma, Manoj Kumar Jonnalagadda, Sreekantha Babu Gundla, Rambabu Antiproliferative Activity of New Pyrazole-4-sulfonamide Derivatives: Synthesis and Biological Evaluation |
title | Antiproliferative
Activity of New Pyrazole-4-sulfonamide
Derivatives: Synthesis and Biological Evaluation |
title_full | Antiproliferative
Activity of New Pyrazole-4-sulfonamide
Derivatives: Synthesis and Biological Evaluation |
title_fullStr | Antiproliferative
Activity of New Pyrazole-4-sulfonamide
Derivatives: Synthesis and Biological Evaluation |
title_full_unstemmed | Antiproliferative
Activity of New Pyrazole-4-sulfonamide
Derivatives: Synthesis and Biological Evaluation |
title_short | Antiproliferative
Activity of New Pyrazole-4-sulfonamide
Derivatives: Synthesis and Biological Evaluation |
title_sort | antiproliferative
activity of new pyrazole-4-sulfonamide
derivatives: synthesis and biological evaluation |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10373183/ https://www.ncbi.nlm.nih.gov/pubmed/37521676 http://dx.doi.org/10.1021/acsomega.2c07539 |
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