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Benign Synthesis of Fused-thiazoles with Enone-based Natural Products and Drugs for Lead Discovery.
Alnufaie, Rawan; Ali, Mohamad Akbar; Alkhaibari, Ibrahim S; Roy, Subrata; Day, Victor W; Alam, Mohammad A.
Afiliación
  • Alnufaie R; Department of Chemistry and Physics, College of Science and Mathematics, Arkansas State University, Jonesboro, Arkansas 72467, United States.
  • Ali MA; Department of Chemistry, College of Science, King Faisal University, Al-Ahsa 31982, Saudi Arabia.
  • Alkhaibari IS; Department of Chemistry and Physics, College of Science and Mathematics, Arkansas State University, Jonesboro, Arkansas 72467, United States.
  • Roy S; Department of Chemistry and Physics, College of Science and Mathematics, Arkansas State University, Jonesboro, Arkansas 72467, United States.
  • Day VW; Department of Chemistry, Integrated Science Building, University of Kansas, Lawrence, Kansas 66046, United States.
  • Alam MA; Department of Chemistry and Physics, College of Science and Mathematics, Arkansas State University, Jonesboro, Arkansas 72467, United States.
New J Chem ; 45(13): 6001-6017, 2021 Apr 07.
Article en En | MEDLINE | ID: mdl-33840994
In an effort to synthesize a library of bioactive molecules, we present an efficient synthesis of fused-thiazole derivatives of natural products and approved drugs by using an environmentally usable solvent, acetic acid, and without any external reagent. Cholestenone, ethisterone, progesterone, and nootkatone-derived epoxyketones have been utilized to synthesize 50 novel compounds. The plausible mechanism of the reaction has been determined by theoretical calculation using M06-2X/6-31+G(d,p). These novel molecules have been tested against cancer cell lines and pathogenic bacterial strains. Several ethisterone-based fused-thiazole compounds are found to be potent growth inhibitors of cancer cell lines at submicromolar concentrations.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Idioma: En Revista: New J Chem Año: 2021 Tipo del documento: Article País de afiliación: Estados Unidos Pais de publicación: Reino Unido
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Idioma: En Revista: New J Chem Año: 2021 Tipo del documento: Article País de afiliación: Estados Unidos Pais de publicación: Reino Unido