Unknown

Dataset Information

0

Biological evaluation, docking studies, and in silico ADME prediction of some pyrimidine and pyridine derivatives as potential EGFRWT and EGFRT790M inhibitors.


ABSTRACT: 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.

SUBMITTER: Al-Warhi T 

PROVIDER: S-EPMC9635468 | biostudies-literature | 2023 Dec

REPOSITORIES: biostudies-literature

altmetric image

Publications

Biological evaluation, docking studies, and <i>in silico</i> ADME prediction of some pyrimidine and pyridine derivatives as potential EGFR<sup>WT</sup> and EGFR<sup>T790M</sup> inhibitors.

Al-Warhi Tarfah T   Al-Karmalawy Ahmed A AA   Elmaaty Ayman Abo AA   Alshubramy Maha A MA   Abdel-Motaal Marwa M   Majrashi Taghreed A TA   Asem Medhat M   Nabil Ahmed A   Eldehna Wagdy M WM   Sharaky Marwa M  

Journal of enzyme inhibition and medicinal chemistry 20231201 1


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 <b>8</b> and <b>14</b> displayed outstanding effects on the investigated cell lines and were further tested for their antioxidant activity in MCF7, H460, FADU, HEP  ...[more]

Similar Datasets

| S-EPMC9466626 | biostudies-literature
| S-EPMC11378702 | biostudies-literature
| S-EPMC8892849 | biostudies-literature
| S-EPMC9500845 | biostudies-literature
| S-EPMC9067978 | biostudies-literature
| S-EPMC10620772 | biostudies-literature
| S-EPMC10150624 | biostudies-literature
| S-EPMC10408569 | biostudies-literature
| S-EPMC9674911 | biostudies-literature
| S-EPMC9609714 | biostudies-literature