In vitro anti-BK polyomavirus activity of imidazo[1,2-c]pyrimidine and pyrimido[1,6 a]pyrimidine derivatives
Five imidazo[1,2-c]pyrimidine and pyrimido[1,6-a]pyrimidine derivatives were designed, synthesized and evaluated for their antiproliferative activity and cytotoxicity. Primary bioassays in vitro showed that two of five synthesized compounds, 6-benzyl-8-(methylsulfonyl)-2,6-dihydroimidazo[1,2-c]pyrim...
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| Format: | Article |
| Language: | English |
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Growing Science
2019-10-01
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| Series: | Current Chemistry Letters |
| Subjects: | |
| Online Access: | http://www.growingscience.com/ccl/Vol9/ccl_2019_29.pdf |
| _version_ | 1818483265543077888 |
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| author | Roman Solomyannyi Oleg Mitiukhin Mark Prichard Scott James Carol Hartline Victor Zhirnov Volodymyr Brovarets |
| author_facet | Roman Solomyannyi Oleg Mitiukhin Mark Prichard Scott James Carol Hartline Victor Zhirnov Volodymyr Brovarets |
| author_sort | Roman Solomyannyi |
| collection | DOAJ |
| description | Five imidazo[1,2-c]pyrimidine and pyrimido[1,6-a]pyrimidine derivatives were designed, synthesized and evaluated for their antiproliferative activity and cytotoxicity. Primary bioassays in vitro showed that two of five synthesized compounds, 6-benzyl-8-(methylsulfonyl)-2,6-dihydroimidazo[1,2-c]pyrimidin-5(3H)-one, and 9-(methylsulfonyl)-7-propyl-2,3,4,7-tetrahydro-6H-pyrimido[1,6-a]pyrimidin-6-one possessed potent antiviral activity against BKV (EC50: 0.66 μM and 0.96, respectively). The selectivity index of these compounds is similar to that of cidofovir. Although antiviral activity was evident in secondary assays, significant virus inhibition occurred at or near the cytotoxic concentration (SI90=1). Here we show that substituted pyrimidine derivatives are a promising structure class of chemical compounds for the development of antiviral drugs against BKV infections. Hence these compounds may be taken as lead compounds for further development of novel antimicrobial and anticancer agents. |
| first_indexed | 2024-12-10T11:58:00Z |
| format | Article |
| id | doaj.art-82e5851a802f4d008d0772448f1877e1 |
| institution | Directory Open Access Journal |
| issn | 1927-7296 1927-730X |
| language | English |
| last_indexed | 2024-12-10T11:58:00Z |
| publishDate | 2019-10-01 |
| publisher | Growing Science |
| record_format | Article |
| series | Current Chemistry Letters |
| spelling | doaj.art-82e5851a802f4d008d0772448f1877e12022-12-22T01:49:42ZengGrowing ScienceCurrent Chemistry Letters1927-72961927-730X2019-10-0192899610.5267/j.ccl.2019.9.001In vitro anti-BK polyomavirus activity of imidazo[1,2-c]pyrimidine and pyrimido[1,6 a]pyrimidine derivativesRoman SolomyannyiOleg MitiukhinMark PrichardScott JamesCarol HartlineVictor ZhirnovVolodymyr BrovaretsFive imidazo[1,2-c]pyrimidine and pyrimido[1,6-a]pyrimidine derivatives were designed, synthesized and evaluated for their antiproliferative activity and cytotoxicity. Primary bioassays in vitro showed that two of five synthesized compounds, 6-benzyl-8-(methylsulfonyl)-2,6-dihydroimidazo[1,2-c]pyrimidin-5(3H)-one, and 9-(methylsulfonyl)-7-propyl-2,3,4,7-tetrahydro-6H-pyrimido[1,6-a]pyrimidin-6-one possessed potent antiviral activity against BKV (EC50: 0.66 μM and 0.96, respectively). The selectivity index of these compounds is similar to that of cidofovir. Although antiviral activity was evident in secondary assays, significant virus inhibition occurred at or near the cytotoxic concentration (SI90=1). Here we show that substituted pyrimidine derivatives are a promising structure class of chemical compounds for the development of antiviral drugs against BKV infections. Hence these compounds may be taken as lead compounds for further development of novel antimicrobial and anticancer agents.http://www.growingscience.com/ccl/Vol9/ccl_2019_29.pdfAntiviral activitypyrimidine derivativesBK polyomavirusheterocyclescyclizatio |
| spellingShingle | Roman Solomyannyi Oleg Mitiukhin Mark Prichard Scott James Carol Hartline Victor Zhirnov Volodymyr Brovarets In vitro anti-BK polyomavirus activity of imidazo[1,2-c]pyrimidine and pyrimido[1,6 a]pyrimidine derivatives Current Chemistry Letters Antiviral activity pyrimidine derivatives BK polyomavirus heterocycles cyclizatio |
| title | In vitro anti-BK polyomavirus activity of imidazo[1,2-c]pyrimidine and pyrimido[1,6 a]pyrimidine derivatives |
| title_full | In vitro anti-BK polyomavirus activity of imidazo[1,2-c]pyrimidine and pyrimido[1,6 a]pyrimidine derivatives |
| title_fullStr | In vitro anti-BK polyomavirus activity of imidazo[1,2-c]pyrimidine and pyrimido[1,6 a]pyrimidine derivatives |
| title_full_unstemmed | In vitro anti-BK polyomavirus activity of imidazo[1,2-c]pyrimidine and pyrimido[1,6 a]pyrimidine derivatives |
| title_short | In vitro anti-BK polyomavirus activity of imidazo[1,2-c]pyrimidine and pyrimido[1,6 a]pyrimidine derivatives |
| title_sort | in vitro anti bk polyomavirus activity of imidazo 1 2 c pyrimidine and pyrimido 1 6 a pyrimidine derivatives |
| topic | Antiviral activity pyrimidine derivatives BK polyomavirus heterocycles cyclizatio |
| url | http://www.growingscience.com/ccl/Vol9/ccl_2019_29.pdf |
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