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Thiophene Derivatives as New Anticancer Agents and Their Therapeutic Delivery Using Folate Receptor-Targeting Nanocarriers
[Image: see text] A series of thiophene derivatives were synthesized by functionalization of 2,3-fused thiophene scaffolds. Their cytotoxicity was assessed against HeLa and Hep G2 cells. Compound 480 was identified as a promising candidate because of its low IC(50) in HeLa (12.61 μg/mL) and Hep G2 (...
Autores principales: | , , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
American Chemical Society
2019
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Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6648408/ https://www.ncbi.nlm.nih.gov/pubmed/31459975 http://dx.doi.org/10.1021/acsomega.9b00554 |
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author | Zhao, Menghui Cui, Yaxin Zhao, Lang Zhu, Tianyu Lee, Robert J. Liao, Weiwei Sun, Fengying Li, Youxin Teng, Lesheng |
author_facet | Zhao, Menghui Cui, Yaxin Zhao, Lang Zhu, Tianyu Lee, Robert J. Liao, Weiwei Sun, Fengying Li, Youxin Teng, Lesheng |
author_sort | Zhao, Menghui |
collection | PubMed |
description | [Image: see text] A series of thiophene derivatives were synthesized by functionalization of 2,3-fused thiophene scaffolds. Their cytotoxicity was assessed against HeLa and Hep G2 cells. Compound 480 was identified as a promising candidate because of its low IC(50) in HeLa (12.61 μg/mL) and Hep G2 (33.42 μg/mL) cells. The drug was loaded into folic acid (FA)-coated nanoparticles (NPs) to address its poor water solubility and to improve its selectivity for cancer cells. Compound 480 was shown to induce apoptosis by changes in mitochondrial membrane potential (ΔΨ(m)) and the reactive oxygen species level. Furthermore, FA-modified NPs enhanced uptake capacity compared to unmodified controls by flow cytometry. This drug delivered in folate nanocarriers is promising for the treatment of cancers. |
format | Online Article Text |
id | pubmed-6648408 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2019 |
publisher | American Chemical Society |
record_format | MEDLINE/PubMed |
spelling | pubmed-66484082019-08-27 Thiophene Derivatives as New Anticancer Agents and Their Therapeutic Delivery Using Folate Receptor-Targeting Nanocarriers Zhao, Menghui Cui, Yaxin Zhao, Lang Zhu, Tianyu Lee, Robert J. Liao, Weiwei Sun, Fengying Li, Youxin Teng, Lesheng ACS Omega [Image: see text] A series of thiophene derivatives were synthesized by functionalization of 2,3-fused thiophene scaffolds. Their cytotoxicity was assessed against HeLa and Hep G2 cells. Compound 480 was identified as a promising candidate because of its low IC(50) in HeLa (12.61 μg/mL) and Hep G2 (33.42 μg/mL) cells. The drug was loaded into folic acid (FA)-coated nanoparticles (NPs) to address its poor water solubility and to improve its selectivity for cancer cells. Compound 480 was shown to induce apoptosis by changes in mitochondrial membrane potential (ΔΨ(m)) and the reactive oxygen species level. Furthermore, FA-modified NPs enhanced uptake capacity compared to unmodified controls by flow cytometry. This drug delivered in folate nanocarriers is promising for the treatment of cancers. American Chemical Society 2019-05-22 /pmc/articles/PMC6648408/ /pubmed/31459975 http://dx.doi.org/10.1021/acsomega.9b00554 Text en Copyright © 2019 American Chemical Society This is an open access article published under an ACS AuthorChoice License (http://pubs.acs.org/page/policy/authorchoice_termsofuse.html) , which permits copying and redistribution of the article or any adaptations for non-commercial purposes. |
spellingShingle | Zhao, Menghui Cui, Yaxin Zhao, Lang Zhu, Tianyu Lee, Robert J. Liao, Weiwei Sun, Fengying Li, Youxin Teng, Lesheng Thiophene Derivatives as New Anticancer Agents and Their Therapeutic Delivery Using Folate Receptor-Targeting Nanocarriers |
title | Thiophene Derivatives as New Anticancer Agents and
Their Therapeutic Delivery Using Folate Receptor-Targeting Nanocarriers |
title_full | Thiophene Derivatives as New Anticancer Agents and
Their Therapeutic Delivery Using Folate Receptor-Targeting Nanocarriers |
title_fullStr | Thiophene Derivatives as New Anticancer Agents and
Their Therapeutic Delivery Using Folate Receptor-Targeting Nanocarriers |
title_full_unstemmed | Thiophene Derivatives as New Anticancer Agents and
Their Therapeutic Delivery Using Folate Receptor-Targeting Nanocarriers |
title_short | Thiophene Derivatives as New Anticancer Agents and
Their Therapeutic Delivery Using Folate Receptor-Targeting Nanocarriers |
title_sort | thiophene derivatives as new anticancer agents and
their therapeutic delivery using folate receptor-targeting nanocarriers |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6648408/ https://www.ncbi.nlm.nih.gov/pubmed/31459975 http://dx.doi.org/10.1021/acsomega.9b00554 |
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