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Exploring novel nitrofuranyl sulfonohydrazides as anti‐Leishmania and anti‐cancer agents: Synthesis, in vitro efficacy and hit identification
Leishmaniasis and cancer are two deadly diseases that plague the human population. There are a limited number of drugs available for the treatment of these diseases; however, their overuse has resulted in pathogenic resistance. Recent studies have indicated the repurposing of nitro‐containing compou...
Autores principales: | , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
John Wiley and Sons Inc.
2022
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9546217/ https://www.ncbi.nlm.nih.gov/pubmed/35648075 http://dx.doi.org/10.1111/cbdd.14097 |
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author | Kannigadu, Christina Aucamp, Janine N'Da, David D. |
author_facet | Kannigadu, Christina Aucamp, Janine N'Da, David D. |
author_sort | Kannigadu, Christina |
collection | PubMed |
description | Leishmaniasis and cancer are two deadly diseases that plague the human population. There are a limited number of drugs available for the treatment of these diseases; however, their overuse has resulted in pathogenic resistance. Recent studies have indicated the repurposing of nitro‐containing compounds to be a new avenue into finding new treatments. In this study, new nitrofuranyl sulfonohydrazide derivatives were synthesized and evaluated for their in vitro antileishmanial and anticancer activities. The analogue 2h, featuring biphenyl moiety exhibited selective (SI > 10) submicromolar activity (IC(50) 0.97 μM) against acute promyelocytic leukemia cells hence was identified anticancer hit. This study revealed no antileishmanial hit. However, several promising analogues were uncovered and are worthy of further structural modifications to improve their toxicity and bioactivity profiles. |
format | Online Article Text |
id | pubmed-9546217 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2022 |
publisher | John Wiley and Sons Inc. |
record_format | MEDLINE/PubMed |
spelling | pubmed-95462172022-10-14 Exploring novel nitrofuranyl sulfonohydrazides as anti‐Leishmania and anti‐cancer agents: Synthesis, in vitro efficacy and hit identification Kannigadu, Christina Aucamp, Janine N'Da, David D. Chem Biol Drug Des Research Articles Leishmaniasis and cancer are two deadly diseases that plague the human population. There are a limited number of drugs available for the treatment of these diseases; however, their overuse has resulted in pathogenic resistance. Recent studies have indicated the repurposing of nitro‐containing compounds to be a new avenue into finding new treatments. In this study, new nitrofuranyl sulfonohydrazide derivatives were synthesized and evaluated for their in vitro antileishmanial and anticancer activities. The analogue 2h, featuring biphenyl moiety exhibited selective (SI > 10) submicromolar activity (IC(50) 0.97 μM) against acute promyelocytic leukemia cells hence was identified anticancer hit. This study revealed no antileishmanial hit. However, several promising analogues were uncovered and are worthy of further structural modifications to improve their toxicity and bioactivity profiles. John Wiley and Sons Inc. 2022-06-21 2022-08 /pmc/articles/PMC9546217/ /pubmed/35648075 http://dx.doi.org/10.1111/cbdd.14097 Text en © 2022 The Authors. Chemical Biology & Drug Design published by John Wiley & Sons Ltd. https://creativecommons.org/licenses/by/4.0/This is an open access article under the terms of the http://creativecommons.org/licenses/by/4.0/ (https://creativecommons.org/licenses/by/4.0/) License, which permits use, distribution and reproduction in any medium, provided the original work is properly cited. |
spellingShingle | Research Articles Kannigadu, Christina Aucamp, Janine N'Da, David D. Exploring novel nitrofuranyl sulfonohydrazides as anti‐Leishmania and anti‐cancer agents: Synthesis, in vitro efficacy and hit identification |
title | Exploring novel nitrofuranyl sulfonohydrazides as anti‐Leishmania and anti‐cancer agents: Synthesis, in vitro efficacy and hit identification |
title_full | Exploring novel nitrofuranyl sulfonohydrazides as anti‐Leishmania and anti‐cancer agents: Synthesis, in vitro efficacy and hit identification |
title_fullStr | Exploring novel nitrofuranyl sulfonohydrazides as anti‐Leishmania and anti‐cancer agents: Synthesis, in vitro efficacy and hit identification |
title_full_unstemmed | Exploring novel nitrofuranyl sulfonohydrazides as anti‐Leishmania and anti‐cancer agents: Synthesis, in vitro efficacy and hit identification |
title_short | Exploring novel nitrofuranyl sulfonohydrazides as anti‐Leishmania and anti‐cancer agents: Synthesis, in vitro efficacy and hit identification |
title_sort | exploring novel nitrofuranyl sulfonohydrazides as anti‐leishmania and anti‐cancer agents: synthesis, in vitro efficacy and hit identification |
topic | Research Articles |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9546217/ https://www.ncbi.nlm.nih.gov/pubmed/35648075 http://dx.doi.org/10.1111/cbdd.14097 |
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