Literature DB >> 16360193

Parallel synthesis of 5-cyano-6-aryl-2-thiouracil derivatives as inhibitors for hepatitis C viral NS5B RNA-dependent RNA polymerase.

Yili Ding1, Jean-Luc Girardet, Kenneth L Smith, Gary Larson, Brett Prigaro, Jim Z Wu, Nanhua Yao.   

Abstract

From random screening of our compound libraries, we identified a hit compound with an IC50 of 27 microM against hepatitis C viral NS5B RNA-dependent RNA polymerase. By using a parallel synthetic strategy, a series of its derivatives were synthesized. From their anti-HCV activity screening, compounds with single digital 3.8 micromolar activity were obtained.

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Year:  2005        PMID： 16360193     DOI： 10.1016/j.bioorg.2005.10.001

Source DB:  PubMed          Journal:  Bioorg Chem        ISSN： 0045-2068            Impact factor:   5.275


  11 in total

1.  Synthesis, characterization and molecular docking studies of thiouracil derivatives as potent thymidylate synthase inhibitors and potential anticancer agents.

Authors:  Abeer M El-Naggar; Mohsen M Abou-El-Regal; Souad A El-Metwally; Farag F Sherbiny; Ibrahim H Eissa
Journal:  Mol Divers       Date:  2017-08-16       Impact factor: 2.943

2.  Novel cyanothiouracil and cyanothiocytosine derivatives as concentration-dependent selective inhibitors of U87MG glioblastomas: Adenosine receptor binding and potent PDE4 inhibition.

Authors:  Zafer Sahin; Sevde Nur Biltekin; Leyla Yurttas; Barkin Berk; Yağmur Özhan; Hande Sipahi; Zhan-Guo Gao; Kenneth A Jacobson; Şeref Demirayak
Journal:  Eur J Med Chem       Date:  2020-12-31       Impact factor: 6.514

3.  2-[(4-Chloro-benz-yl)sulfan-yl]-4-(2-methyl-prop-yl)-6-(phenyl-sulfan-yl)pyrimidine-5-carbonitrile.

Authors:  Ali A El-Emam; Omar A Al-Deeb; Abdulghafoor A Al-Turkistani; Seik Weng Ng; Edward R T Tiekink
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2012-06-13

4.  6-(2-Methyl-prop-yl)-4-oxo-2-sulfanyl-idene-1,2,3,4-tetra-hydro-pyrimidine-5-carbonitrile.

Authors:  Omar A Al-Deeb; Ali A El-Emam; Abdulghafoor A Al-Turkistani; Seik Weng Ng; Edward R T Tiekink
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2012-02-10

5.  2-[(4-Chloro-benz-yl)sulfanyl]-4-(2-methyl-prop-yl)-6-[3-(trifluoro-meth-yl)anilino]-pyrimidine-5-carbonitrile.

Authors:  Ali A El-Emam; Omar A Al-Deeb; Nasser R El-Brollosy; Seik Weng Ng; Edward R T Tiekink
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2012-06-13

6.  One pot synthesis, antimicrobial and antioxidant activities of fused uracils: pyrimidodiazepines, lumazines, triazolouracil and xanthines.

Authors:  Samar A El-Kalyoubi; Eman A Fayed; Ahmed S Abdel-Razek
Journal:  Chem Cent J       Date:  2017-07-19       Impact factor: 4.215

7.  Synthesis and antimicrobial activity of some novel 5-alkyl-6-substituted uracils and related derivatives.

Authors:  Abdulghafoor A Al-Turkistani; Omar A Al-Deeb; Nasser R El-Brollosy; Ali A El-Emam
Journal:  Molecules       Date:  2011-06-08       Impact factor: 4.411

8.  Novel adenosine derivatives against SARS-CoV-2 RNA-dependent RNA polymerase: an in silico perspective.

Authors:  Amr Sonousi; Hanan A Mahran; Ibrahim M Ibrahim; Mohamed N Ibrahim; Abdo A Elfiky; Wael M Elshemey
Journal:  Pharmacol Rep       Date:  2021-06-24       Impact factor: 3.919

9.  Synthesis, antifungal activity, and QSAR studies of 1,6-dihydropyrimidine derivatives.

Authors:  Chirag Rami; Laxmanbhai Patel; Chhaganbhai N Patel; Jayshree P Parmar
Journal:  J Pharm Bioallied Sci       Date:  2013-10

10.  Synthesis and bioactivity evaluation of new 6-aryl-5-cyano thiouracils as potential antimicrobial and anticancer agents.

Authors:  Azza Taher Taher; Sahar Mahmoud Abou-Seri
Journal:  Molecules       Date:  2012-08-17       Impact factor: 4.411
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