Your browser doesn't support javascript.
loading
Biological evaluation, docking studies, and in silico ADME prediction of some pyrimidine and pyridine derivatives as potential EGFRWT and EGFRT790M inhibitors.
Al-Warhi, Tarfah; Al-Karmalawy, Ahmed A; Elmaaty, Ayman Abo; Alshubramy, Maha A; Abdel-Motaal, Marwa; Majrashi, Taghreed A; Asem, Medhat; Nabil, Ahmed; Eldehna, Wagdy M; Sharaky, Marwa.
Afiliação
  • Al-Warhi T; Department of Chemistry, College of Science, Princess Nourah bint Abdulrahman University, Riyadh, Saudi Arabia.
  • Al-Karmalawy AA; Pharmaceutical Chemistry Department, Faculty of Pharmacy, Ahram Canadian University, Giza, Egypt.
  • Elmaaty AA; Department of Medicinal Chemistry, Faculty of Pharmacy, Port Said University, Port Said, Egypt.
  • Alshubramy MA; Department of Chemistry, College of Science, Qassim University, Buraydah, Saudi Arabia.
  • Abdel-Motaal M; Department of Chemistry, College of Science, Qassim University, Buraydah, Saudi Arabia.
  • Majrashi TA; Chemistry Department, Faculty of Science, Mansoura University, Mansoura, Egypt.
  • Asem M; Department of Pharmacognosy, College of Pharmacy, King Khalid University, Abha, Saudi Arabia.
  • Nabil A; College of Engineering and Information Technology, Onaizah Colleges, Al-Qassim, Saudi Arabia.
  • Eldehna WM; Research Center for Functional Materials, National Institute for Materials Science (NIMS), Tsukuba, Japan.
  • Sharaky M; Biotechnology and Life Sciences Department, Faculty of Postgraduate Studies for Advanced Sciences (PSAS), Beni-Suef University, Beni-Suef, Egypt.
J Enzyme Inhib Med Chem ; 38(1): 176-191, 2023 Dec.
Article em En | MEDLINE | ID: mdl-36317648
Herein, a set of pyridine and pyrimidine derivatives were assessed for their impact on the cell cycle and apoptosis. Human breast cancer (MCF7), hepatocellular carcinoma (HEPG2), larynx cancer (HEP2), lung cancer (H460), colon cancers (HCT116 and Caco2), and hypopharyngeal cancer (FADU), and normal Vero cell lines were used. Compounds 8 and 14 displayed outstanding effects on the investigated cell lines and were further tested for their antioxidant activity in MCF7, H460, FADU, HEP2, HEPG2, HCT116, Caco2, and Vero cells by measuring superoxide dismutase (SOD), malondialdehyde content (MDA), reduced glutathione (GSH), and nitric oxide (NO) content. Besides, Annexin V-FITC apoptosis detection and cell cycle DNA index using the HEPG-2 cell line were established on both compounds as well. Furthermore, compounds 8 and 14 were assessed for their EGFR kinase (Wild and T790M) inhibitory activities, revealing eligible potential. Additionally, molecular docking, ADME, and SAR studies were carried out for the investigated candidates.
Assuntos
Palavras-chave

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Neoplasias Pulmonares / Antineoplásicos Limite: Animals / Humans Idioma: En Revista: J Enzyme Inhib Med Chem Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2023 Tipo de documento: Article País de afiliação: Arábia Saudita País de publicação: Reino Unido

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Neoplasias Pulmonares / Antineoplásicos Limite: Animals / Humans Idioma: En Revista: J Enzyme Inhib Med Chem Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2023 Tipo de documento: Article País de afiliação: Arábia Saudita País de publicação: Reino Unido