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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...

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Autores principales: Mahesh, Panasa, Akshinthala, Parameswari, Katari, Naresh Kumar, Gupta, Lavleen Kumar, Panwar, Dikshita, Sharma, Manoj Kumar, Jonnalagadda, Sreekantha Babu, Gundla, Rambabu
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2023
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.
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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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