α,α-Difluoro-β-ketophosphonates on a tetraazamacrocyclic platform: Synthesis and inhibitory activity against protein tyrosine phosphatases

The present study offers a new approach for designing inhibitors of protein tyrosine phosphatases. We have synthesized the cyclam derivatives with α,α-difluoro-β-ketophosphonate fragments covalently attached to tetraazamacrocyclic scaffold, which is known to be of medical interest. The obtained fu...

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Published in:Доповіді НАН України
Date:2014
Main Authors: Khavrienko, D.I., Kobzar, O.L., Shevchuk, M.V., Romanenko, V.D., Kobelev, S.M., Averin, A.D., Beletskaya, I.P., Vovk, A.I., Kukhar, V.P.
Format: Article
Language:English
Published: Видавничий дім "Академперіодика" НАН України 2014
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Online Access:https://nasplib.isofts.kiev.ua/handle/123456789/88260
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Journal Title:Digital Library of Periodicals of National Academy of Sciences of Ukraine
Cite this:α,α-Difluoro-β-ketophosphonates on a tetraazamacrocyclic platform: Synthesis and inhibitory activity against protein tyrosine phosphatases / D.I. Khavrienko, O.L. Kobzar, M.V. Shevchuk, V.D. Romanenko, S.M. Kobelev, A.D. Averin, I.P. Beletskaya, A.I. Vovk, V.P. Kukhar // Доповiдi Нацiональної академiї наук України. — 2014. — № 9. — С. 109-115. — Бібліогр.: 15 назв. — англ.

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Digital Library of Periodicals of National Academy of Sciences of Ukraine
id nasplib_isofts_kiev_ua-123456789-88260
record_format dspace
spelling Khavrienko, D.I.
Kobzar, O.L.
Shevchuk, M.V.
Romanenko, V.D.
Kobelev, S.M.
Averin, A.D.
Beletskaya, I.P.
Vovk, A.I.
Kukhar, V.P.
2015-11-11T15:37:45Z
2015-11-11T15:37:45Z
2014
α,α-Difluoro-β-ketophosphonates on a tetraazamacrocyclic platform: Synthesis and inhibitory activity against protein tyrosine phosphatases / D.I. Khavrienko, O.L. Kobzar, M.V. Shevchuk, V.D. Romanenko, S.M. Kobelev, A.D. Averin, I.P. Beletskaya, A.I. Vovk, V.P. Kukhar // Доповiдi Нацiональної академiї наук України. — 2014. — № 9. — С. 109-115. — Бібліогр.: 15 назв. — англ.
1025-6415
https://nasplib.isofts.kiev.ua/handle/123456789/88260
547.241+577.152.3
The present study offers a new approach for designing inhibitors of protein tyrosine phosphatases. We have synthesized the cyclam derivatives with α,α-difluoro-β-ketophosphonate fragments covalently attached to tetraazamacrocyclic scaffold, which is known to be of medical interest. The obtained functionalized macrocycles were evaluated as inhibitors of PTP1B, TC-PTP, CD45, and other protein tyrosine phosphatases.
Запроновано новий пiдхiд до розробки iнгiбiторiв протеїнтирозинфосфатаз. Синтезовано похiднi цикламу з α,α-дифторо-β-кетофосфонатними фрагментами, ковалентно зв’язаними з тетраазамакроциклiчною платформою. Отриманi функцiоналiзованi макроцикли було дослiджено як iнгiбiтори PTP1B, TC-PTP, CD45 та iнших протеїнтирозинфосфатаз.
Предложен новый поход к разработке ингибиторов протеинтирозинфосфатаз. Синтезированы производные циклама с α,α-дифтор-β-кетофосфонатными фрагментами, ковалентно связанными с тетраазамакроциклической платформой. Полученные функционализированные макроциклы были изучены в качестве ингибиторов PTP1B, TC-PTP, CD45 и других протеинтирозинфосфатаз.
This study was financially supported by the State Fund of Fundamental Research of Ukraine (project F53.3/020) and by the National Academy of Sciences of Ukraine (project 01–2/2014). The authors thank D.Yu. Masich for the participation in the synthesis of some compounds.
en
Видавничий дім "Академперіодика" НАН України
Доповіді НАН України
Хімія
α,α-Difluoro-β-ketophosphonates on a tetraazamacrocyclic platform: Synthesis and inhibitory activity against protein tyrosine phosphatases
α,α-Дифторо-β-кетофосфонати на тетраазамакроциклiчнiй платформi: синтез та iнгiбiторна активнiсть по вiдношенню до протеїнтирозинфосфатаз
α,α-Дифтор-β-кетофосфонаты на тетраазамакроциклической платформе: синтез и ингибиторная активность по отношению к протеинтирозинфосфатазам
Article
published earlier
institution Digital Library of Periodicals of National Academy of Sciences of Ukraine
collection DSpace DC
title α,α-Difluoro-β-ketophosphonates on a tetraazamacrocyclic platform: Synthesis and inhibitory activity against protein tyrosine phosphatases
spellingShingle α,α-Difluoro-β-ketophosphonates on a tetraazamacrocyclic platform: Synthesis and inhibitory activity against protein tyrosine phosphatases
Khavrienko, D.I.
Kobzar, O.L.
Shevchuk, M.V.
Romanenko, V.D.
Kobelev, S.M.
Averin, A.D.
Beletskaya, I.P.
Vovk, A.I.
Kukhar, V.P.
Хімія
title_short α,α-Difluoro-β-ketophosphonates on a tetraazamacrocyclic platform: Synthesis and inhibitory activity against protein tyrosine phosphatases
title_full α,α-Difluoro-β-ketophosphonates on a tetraazamacrocyclic platform: Synthesis and inhibitory activity against protein tyrosine phosphatases
title_fullStr α,α-Difluoro-β-ketophosphonates on a tetraazamacrocyclic platform: Synthesis and inhibitory activity against protein tyrosine phosphatases
title_full_unstemmed α,α-Difluoro-β-ketophosphonates on a tetraazamacrocyclic platform: Synthesis and inhibitory activity against protein tyrosine phosphatases
title_sort α,α-difluoro-β-ketophosphonates on a tetraazamacrocyclic platform: synthesis and inhibitory activity against protein tyrosine phosphatases
author Khavrienko, D.I.
Kobzar, O.L.
Shevchuk, M.V.
Romanenko, V.D.
Kobelev, S.M.
Averin, A.D.
Beletskaya, I.P.
Vovk, A.I.
Kukhar, V.P.
author_facet Khavrienko, D.I.
Kobzar, O.L.
Shevchuk, M.V.
Romanenko, V.D.
Kobelev, S.M.
Averin, A.D.
Beletskaya, I.P.
Vovk, A.I.
Kukhar, V.P.
topic Хімія
topic_facet Хімія
publishDate 2014
language English
container_title Доповіді НАН України
publisher Видавничий дім "Академперіодика" НАН України
format Article
title_alt α,α-Дифторо-β-кетофосфонати на тетраазамакроциклiчнiй платформi: синтез та iнгiбiторна активнiсть по вiдношенню до протеїнтирозинфосфатаз
α,α-Дифтор-β-кетофосфонаты на тетраазамакроциклической платформе: синтез и ингибиторная активность по отношению к протеинтирозинфосфатазам
description The present study offers a new approach for designing inhibitors of protein tyrosine phosphatases. We have synthesized the cyclam derivatives with α,α-difluoro-β-ketophosphonate fragments covalently attached to tetraazamacrocyclic scaffold, which is known to be of medical interest. The obtained functionalized macrocycles were evaluated as inhibitors of PTP1B, TC-PTP, CD45, and other protein tyrosine phosphatases. Запроновано новий пiдхiд до розробки iнгiбiторiв протеїнтирозинфосфатаз. Синтезовано похiднi цикламу з α,α-дифторо-β-кетофосфонатними фрагментами, ковалентно зв’язаними з тетраазамакроциклiчною платформою. Отриманi функцiоналiзованi макроцикли було дослiджено як iнгiбiтори PTP1B, TC-PTP, CD45 та iнших протеїнтирозинфосфатаз. Предложен новый поход к разработке ингибиторов протеинтирозинфосфатаз. Синтезированы производные циклама с α,α-дифтор-β-кетофосфонатными фрагментами, ковалентно связанными с тетраазамакроциклической платформой. Полученные функционализированные макроциклы были изучены в качестве ингибиторов PTP1B, TC-PTP, CD45 и других протеинтирозинфосфатаз.
issn 1025-6415
url https://nasplib.isofts.kiev.ua/handle/123456789/88260
citation_txt α,α-Difluoro-β-ketophosphonates on a tetraazamacrocyclic platform: Synthesis and inhibitory activity against protein tyrosine phosphatases / D.I. Khavrienko, O.L. Kobzar, M.V. Shevchuk, V.D. Romanenko, S.M. Kobelev, A.D. Averin, I.P. Beletskaya, A.I. Vovk, V.P. Kukhar // Доповiдi Нацiональної академiї наук України. — 2014. — № 9. — С. 109-115. — Бібліогр.: 15 назв. — англ.
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