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 |
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| Date: | 2014 |
| Main Authors: | , , , , , , , , |
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| Language: | English |
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Видавничий дім "Академперіодика" НАН України
2014
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| Online Access: | https://nasplib.isofts.kiev.ua/handle/123456789/88260 |
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| 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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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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