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Design, synthesis and biological evaluation of 2-quinolyl-1,3-tropolone derivatives as new anti-cancer agents
Tropolones are promising organic compounds that can have important biologic effects. We developed a series of new 2-quinolyl-1,3-tropolones derivatives that were prepared by the acid-catalyzed reaction of 4,7-dichloro-2-methylquinolines with 1,2-benzoquinones. 2-Quinolyl-1,3-tropolones have been syn...
Autores principales: | , , , , , , , , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
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The Royal Society of Chemistry
2021
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8121267/ https://www.ncbi.nlm.nih.gov/pubmed/33996031 http://dx.doi.org/10.1039/d0ra10610k |
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author | Gusakov, Evgeniy A. Topchu, Iuliia A. Mazitova, Aleksandra M. Dorogan, Igor V. Bulatov, Emil R. Serebriiskii, Ilya G. Abramova, Zinaida I. Tupaeva, Inna O. Demidov, Oleg P. Toan, Duong Ngoc Lam, Tran Dai Bang, Duong Nghia Boumber, Yanis A. Sayapin, Yurii A. Minkin, Vladimir I. |
author_facet | Gusakov, Evgeniy A. Topchu, Iuliia A. Mazitova, Aleksandra M. Dorogan, Igor V. Bulatov, Emil R. Serebriiskii, Ilya G. Abramova, Zinaida I. Tupaeva, Inna O. Demidov, Oleg P. Toan, Duong Ngoc Lam, Tran Dai Bang, Duong Nghia Boumber, Yanis A. Sayapin, Yurii A. Minkin, Vladimir I. |
author_sort | Gusakov, Evgeniy A. |
collection | PubMed |
description | Tropolones are promising organic compounds that can have important biologic effects. We developed a series of new 2-quinolyl-1,3-tropolones derivatives that were prepared by the acid-catalyzed reaction of 4,7-dichloro-2-methylquinolines with 1,2-benzoquinones. 2-Quinolyl-1,3-tropolones have been synthesized and tested for their anti-proliferative activity against several human cancer cell lines. Two compounds (3d and mixture B of 3i–k) showed excellent activity against six cancer cell lines of different tissue of origin. The promising compounds 3d and mixture B of 3i–k also demonstrated induction of apoptotic cell death of ovarian cancer (OVCAR-3, OVCAR-8) and colon cancer (HCT 116) cell lines and affected ERK signaling. In summary, 2-quinolyl-1,3-tropolones are promising compounds for development of effective anticancer agents. |
format | Online Article Text |
id | pubmed-8121267 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2021 |
publisher | The Royal Society of Chemistry |
record_format | MEDLINE/PubMed |
spelling | pubmed-81212672021-05-14 Design, synthesis and biological evaluation of 2-quinolyl-1,3-tropolone derivatives as new anti-cancer agents Gusakov, Evgeniy A. Topchu, Iuliia A. Mazitova, Aleksandra M. Dorogan, Igor V. Bulatov, Emil R. Serebriiskii, Ilya G. Abramova, Zinaida I. Tupaeva, Inna O. Demidov, Oleg P. Toan, Duong Ngoc Lam, Tran Dai Bang, Duong Nghia Boumber, Yanis A. Sayapin, Yurii A. Minkin, Vladimir I. RSC Adv Chemistry Tropolones are promising organic compounds that can have important biologic effects. We developed a series of new 2-quinolyl-1,3-tropolones derivatives that were prepared by the acid-catalyzed reaction of 4,7-dichloro-2-methylquinolines with 1,2-benzoquinones. 2-Quinolyl-1,3-tropolones have been synthesized and tested for their anti-proliferative activity against several human cancer cell lines. Two compounds (3d and mixture B of 3i–k) showed excellent activity against six cancer cell lines of different tissue of origin. The promising compounds 3d and mixture B of 3i–k also demonstrated induction of apoptotic cell death of ovarian cancer (OVCAR-3, OVCAR-8) and colon cancer (HCT 116) cell lines and affected ERK signaling. In summary, 2-quinolyl-1,3-tropolones are promising compounds for development of effective anticancer agents. The Royal Society of Chemistry 2021-01-22 /pmc/articles/PMC8121267/ /pubmed/33996031 http://dx.doi.org/10.1039/d0ra10610k Text en This journal is © The Royal Society of Chemistry https://creativecommons.org/licenses/by-nc/3.0/ |
spellingShingle | Chemistry Gusakov, Evgeniy A. Topchu, Iuliia A. Mazitova, Aleksandra M. Dorogan, Igor V. Bulatov, Emil R. Serebriiskii, Ilya G. Abramova, Zinaida I. Tupaeva, Inna O. Demidov, Oleg P. Toan, Duong Ngoc Lam, Tran Dai Bang, Duong Nghia Boumber, Yanis A. Sayapin, Yurii A. Minkin, Vladimir I. Design, synthesis and biological evaluation of 2-quinolyl-1,3-tropolone derivatives as new anti-cancer agents |
title | Design, synthesis and biological evaluation of 2-quinolyl-1,3-tropolone derivatives as new anti-cancer agents |
title_full | Design, synthesis and biological evaluation of 2-quinolyl-1,3-tropolone derivatives as new anti-cancer agents |
title_fullStr | Design, synthesis and biological evaluation of 2-quinolyl-1,3-tropolone derivatives as new anti-cancer agents |
title_full_unstemmed | Design, synthesis and biological evaluation of 2-quinolyl-1,3-tropolone derivatives as new anti-cancer agents |
title_short | Design, synthesis and biological evaluation of 2-quinolyl-1,3-tropolone derivatives as new anti-cancer agents |
title_sort | design, synthesis and biological evaluation of 2-quinolyl-1,3-tropolone derivatives as new anti-cancer agents |
topic | Chemistry |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8121267/ https://www.ncbi.nlm.nih.gov/pubmed/33996031 http://dx.doi.org/10.1039/d0ra10610k |
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