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Designing Potent Anti-Cancer Agents: Synthesis and Molecular Docking Studies of Thieno[2,3-d][1,2,4]triazolo[1,5-a]pyrimidine Derivatives.
Elsenbawy, Eman S M; Alshehri, Zafer S; Babteen, Nouf A; Abdel-Rahman, Adel A-H; El-Manawaty, Mai A; Nossier, Eman S; Arafa, Reem K; Hassan, Nasser A.
Afiliación
  • Elsenbawy ESM; Department of Chemistry, Faculty of Science, Menofia University, Shbien El-Kom 32511, Egypt.
  • Alshehri ZS; Department of Medical Laboratories, College of Applied Medical Sciences, Shaqra University, Dawadmi 19257, Saudi Arabia.
  • Babteen NA; Department of Biochemistry, College of Sciences, University of Jeddah, Jeddah 21577, Saudi Arabia.
  • Abdel-Rahman AA; Department of Chemistry, Faculty of Science, Menofia University, Shbien El-Kom 32511, Egypt.
  • El-Manawaty MA; Department of Pharmacognosy, Pharmaceutical Science Division, National Research Centre, Cairo 12622, Egypt.
  • Nossier ES; Department of Pharmaceutical Medicinal Chemistry and Drug Design, Faculty of Pharmacy (Girls), Al-Azhar University, Cairo 11754, Egypt.
  • Arafa RK; Drug Design and Discovery Laboratory, Biomedical Sciences Program, University of Science and Technology, Zewail City of Science and Technology, Ahmed Zewail Road, October Gardens, Cairo 12578, Egypt.
  • Hassan NA; Synthetic Unit, Department of Photochemistry, Chemical Industries Research Institute, National Research Centre, Cairo 12622, Egypt.
Molecules ; 29(5)2024 Feb 29.
Article en En | MEDLINE | ID: mdl-38474579
ABSTRACT
A new series of thieno[2,3-d][1,2,4]triazolo[1,5-a]pyrimidines was designed and synthesized using readily available starting materials, specifically, ß-enaminoester. Their cytotoxicity was screened against three cancer cell lines, namely, MCF-7, HCT-116, and PC-3. 2-(4-bromophenyl)triazole 10b and 2-(anthracen-9-yl)triazole 10e afforded excellent potency against MCF-7 cell lines (IC50 = 19.4 ± 0.22 and 14.5 ± 0.30 µM, respectively) compared with doxorubicin (IC50 = 40.0 ± 3.9 µM). The latter derivatives 10b and 10e were further subjected to in silico ADME and docking simulation studies against EGFR and PI3K and could serve as ideal leads for additional modification in the field of anticancer research.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Antineoplásicos Límite: Humans Idioma: En Revista: Molecules Asunto de la revista: BIOLOGIA Año: 2024 Tipo del documento: Article País de afiliación: Egipto Pais de publicación: Suiza
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Antineoplásicos Límite: Humans Idioma: En Revista: Molecules Asunto de la revista: BIOLOGIA Año: 2024 Tipo del documento: Article País de afiliación: Egipto Pais de publicación: Suiza