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Development of novel amide-derivatized 2,4-bispyridyl thiophenes as highly potent and selective Dyrk1A inhibitors. Part II: Identification of the cyclopropylamide moiety as a key modification.
Darwish, Sarah S; Abdel-Halim, Mohammad; ElHady, Ahmed K; Salah, Mohamed; Abadi, Ashraf H; Becker, Walter; Engel, Matthias.
Affiliation
  • Darwish SS; Department of Pharmaceutical Chemistry, Faculty of Pharmacy and Biotechnology, German University in Cairo, Cairo, 11835, Egypt.
  • Abdel-Halim M; Department of Pharmaceutical Chemistry, Faculty of Pharmacy and Biotechnology, German University in Cairo, Cairo, 11835, Egypt.
  • ElHady AK; Department of Pharmaceutical Chemistry, Faculty of Pharmacy and Biotechnology, German University in Cairo, Cairo, 11835, Egypt.
  • Salah M; Pharmaceutical and Medicinal Chemistry, Saarland University, Campus C2.3, D-66123, Saarbrücken, Germany.
  • Abadi AH; Department of Pharmaceutical Chemistry, Faculty of Pharmacy and Biotechnology, German University in Cairo, Cairo, 11835, Egypt.
  • Becker W; Institute of Pharmacology and Toxicology, Medical Faculty of the RWTH Aachen University, Wendlingweg 2, 52074, Aachen, Germany.
  • Engel M; Pharmaceutical and Medicinal Chemistry, Saarland University, Campus C2.3, D-66123, Saarbrücken, Germany. Electronic address: ma.engel@mx.uni-saarland.de.
Eur J Med Chem ; 158: 270-285, 2018 Oct 05.
Article in En | MEDLINE | ID: mdl-30223116
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Thiophenes / Protein-Tyrosine Kinases / Protein Serine-Threonine Kinases / Protein Kinase Inhibitors Type of study: Diagnostic_studies Limits: Humans Language: En Journal: Eur J Med Chem Year: 2018 Document type: Article Affiliation country: Egypt Country of publication: France
Fulltext
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Thiophenes / Protein-Tyrosine Kinases / Protein Serine-Threonine Kinases / Protein Kinase Inhibitors Type of study: Diagnostic_studies Limits: Humans Language: En Journal: Eur J Med Chem Year: 2018 Document type: Article Affiliation country: Egypt Country of publication: France