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Development of 5-hydroxybenzothiophene derivatives as multi-kinase inhibitors with potential anti-cancer activity.
Abd El-Rahman, Yara A; Chen, Po-Jen; ElHady, Ahmed K; Chen, Shun-Hua; Lin, Hsin-Chieh; El-Gamil, Dalia S; Aboushady, Youssef; Abadi, Ashraf H; Engel, Matthias; Abdel-Halim, Mohammad.
Afiliación
  • Abd El-Rahman YA; Department of Pharmaceutical Chemistry, Faculty of Pharmacy & Biotechnology, German University in Cairo, Cairo, 11835, Egypt.
  • Chen PJ; Department of Medical Research, E-Da Hospital, I-Shou University, Kaohsiung, 824410, Taiwan.
  • ElHady AK; Graduate Institute of Medicine, I-Shou University, Kaohsiung, 824410, Taiwan.
  • Chen SH; Department of Pharmaceutical Chemistry, Faculty of Pharmacy & Biotechnology, German University in Cairo, Cairo, 11835, Egypt.
  • Lin HC; School of Life & Medical Sciences, University of Hertfordshire hosted by Global Academic Foundation, New Administrative Capital, Cairo, Egypt.
  • El-Gamil DS; School of Nursing, Fooyin University, Kaohsiung, 831301, Taiwan.
  • Aboushady Y; Department of Chinese Medicine, E-Da Cancer Hospital, Kaohsiung, 824410, Taiwan.
  • Abadi AH; Department of Pharmaceutical Chemistry, Faculty of Pharmacy & Biotechnology, German University in Cairo, Cairo, 11835, Egypt.
  • Engel M; Department of Chemistry, Faculty of Pharmacy, Ahram Canadian University, Cairo, 12451, Egypt.
  • Abdel-Halim M; Department of Pharmaceutical Chemistry, Faculty of Pharmacy & Biotechnology, German University in Cairo, Cairo, 11835, Egypt.
Future Med Chem ; 16(12): 1239-1254, 2024.
Article en En | MEDLINE | ID: mdl-38989990
ABSTRACT

Aim:

Chemoresistance in cancer challenges the classical therapeutic strategy of 'one molecule-one target'. To combat this, multi-target therapies that inhibit various cancer-relevant targets simultaneously are proposed. Methods &

results:

We introduce 5-hydroxybenzothiophene derivatives as effective multi-target kinase inhibitors, showing notable growth inhibitory activity across different cancer cell lines. Specifically, compound 16b, featuring a 5-hydroxybenzothiophene hydrazide scaffold, emerged as a potent inhibitor, displaying low IC50 values against key kinases and demonstrating significant anti-cancer effects, particularly against U87MG glioblastoma cells. It induced G2/M cell cycle arrest, apoptosis and inhibited cell migration by modulating apoptotic markers.

Conclusion:

16b represents a promising lead for developing new anti-cancer agents targeting multiple kinases with affinity to the hydroxybenzothiophene core.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Tiofenos / Ensayos de Selección de Medicamentos Antitumorales / Apoptosis / Inhibidores de Proteínas Quinasas / Proliferación Celular / Antineoplásicos Límite: Humans Idioma: En Revista: Future Med Chem Año: 2024 Tipo del documento: Article País de afiliación: Egipto Pais de publicación: Reino Unido
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Tiofenos / Ensayos de Selección de Medicamentos Antitumorales / Apoptosis / Inhibidores de Proteínas Quinasas / Proliferación Celular / Antineoplásicos Límite: Humans Idioma: En Revista: Future Med Chem Año: 2024 Tipo del documento: Article País de afiliación: Egipto Pais de publicación: Reino Unido