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Synthesis, biological evaluation, and molecular docking of new series of antitumor and apoptosis inducers designed as VEGFR-2 inhibitors.
Abdallah, Abdallah E; Mabrouk, Reda R; Al Ward, Maged Mohammed Saleh; Eissa, Sally I; Elkaeed, Eslam B; Mehany, Ahmed B M; Abo-Saif, Mariam A; El-Feky, Ola A; Alesawy, Mohamed S; El-Zahabi, Mohamed Ayman.
Afiliación
  • Abdallah AE; Pharmaceutical Medicinal Chemistry & Drug Design Department, Faculty of Pharmacy (Boys), Al-Azhar University, Cairo, Egypt.
  • Mabrouk RR; Pharmaceutical Medicinal Chemistry & Drug Design Department, Faculty of Pharmacy (Boys), Al-Azhar University, Cairo, Egypt.
  • Al Ward MMS; Pharmaceutical Medicinal Chemistry & Drug Design Department, Faculty of Pharmacy (Boys), Al-Azhar University, Cairo, Egypt.
  • Eissa SI; Department of Pharmaceutical Chemistry, Faculty of Pharmacy (Girls), Al-Azhar University, Cairo, Egypt.
  • Elkaeed EB; Department of Pharmaceutical Sciences, College of Pharmacy, AlMaarefa University, Riyadh, Saudi Arabia.
  • Mehany ABM; Department of Pharmaceutical Sciences, College of Pharmacy, AlMaarefa University, Riyadh, Saudi Arabia.
  • Abo-Saif MA; Zoology Department, Faculty of Science, Al-Azhar University, Cairo, Egypt.
  • El-Feky OA; Biochemistry Department, Faculty of Pharmacy, Tanta university, Tanta, Egypt.
  • Alesawy MS; Biochemistry Department, Faculty of Pharmacy, Tanta university, Tanta, Egypt.
  • El-Zahabi MA; Pharmaceutical Medicinal Chemistry & Drug Design Department, Faculty of Pharmacy (Boys), Al-Azhar University, Cairo, Egypt.
J Enzyme Inhib Med Chem ; 37(1): 573-591, 2022 Dec.
Article en En | MEDLINE | ID: mdl-35012403
Based on quinazoline, quinoxaline, and nitrobenzene scaffolds and on pharmacophoric features of VEGFR-2 inhibitors, 17 novel compounds were designed and synthesised. VEGFR-2 IC50 values ranged from 60.00 to 123.85 nM for the new derivatives compared to 54.00 nM for sorafenib. Compounds 15a, 15b, and 15d showed IC50 from 17.39 to 47.10 µM against human cancer cell lines; hepatocellular carcinoma (HepG2), prostate cancer (PC3), and breast cancer (MCF-7). Meanwhile, the first in terms of VEGFR-2 inhibition was compound 15d which came second with regard to antitumor assay with IC50 = 24.10, 40.90, and 33.40 µM against aforementioned cell lines, respectively. Furthermore, Compound 15d increased apoptosis rate of HepG2 from 1.20 to 12.46% as it significantly increased levels of Caspase-3, BAX, and P53 from 49.6274, 40.62, and 42.84 to 561.427, 395.04, and 415.027 pg/mL, respectively. Moreover, 15d showed IC50 of 253 and 381 nM against HER2 and FGFR, respectively.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Apoptosis / Receptor 2 de Factores de Crecimiento Endotelial Vascular / Inhibidores de Proteínas Quinasas / Simulación del Acoplamiento Molecular / Antineoplásicos Límite: Humans Idioma: En Revista: J Enzyme Inhib Med Chem Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2022 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: Apoptosis / Receptor 2 de Factores de Crecimiento Endotelial Vascular / Inhibidores de Proteínas Quinasas / Simulación del Acoplamiento Molecular / Antineoplásicos Límite: Humans Idioma: En Revista: J Enzyme Inhib Med Chem Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2022 Tipo del documento: Article País de afiliación: Egipto Pais de publicación: Reino Unido