New S- and N-alkyl functionalized bis-1,2,4-Triazolyl-based Derivatives as Potential Dual EGFRWT and EGFRT790M Inhibitors: Synthesis, Anti-proliferative Evaluation, Molecular Docking Study and ADMET Studies DOI

A. M. I. Ahmed,

Moustafa O. Aboelez,

Hend A. A. Ezelarab

et al.

Journal of Molecular Structure, Journal Year: 2024, Volume and Issue: unknown, P. 140720 - 140720

Published: Nov. 1, 2024

Language: Английский

New 2-oxoindole derivatives as multiple PDGFRα/ß and VEGFR-2 tyrosine kinase inhibitors DOI
Hend A. A. Ezelarab, Amer Ali Abd El‐Hafeez, Taha F. S. Ali

et al.

Bioorganic Chemistry, Journal Year: 2024, Volume and Issue: 145, P. 107234 - 107234

Published: Feb. 22, 2024

Language: Английский

Citations

3

Therapeutic Effects of a New Bithiophene against Aluminum -Induced Alzheimer’s Disease in a Rat Model: Pathological and Ultrastructural approach DOI

Kholoud AbdEl-Raouf,

Monir A. El-Ganzuri,

Wael M. El‐Sayed

et al.

Tissue and Cell, Journal Year: 2024, Volume and Issue: 90, P. 102529 - 102529

Published: Aug. 22, 2024

Language: Английский

Citations

2

Novel Scaffolds Based on Bis-thiazole Connected to Quinoxaline or Thienothiophene through 2-Phenoxy-N-arylacetamide Groups as New Hybrid Molecules: Synthesis, Antibacterial Activity, and Molecular Docking Investigations DOI Creative Commons
Mostafa E. Salem,

Abbas H. Abdullah,

Nada S. Ibrahim

et al.

ACS Omega, Journal Year: 2023, Volume and Issue: 8(46), P. 44312 - 44327

Published: Nov. 10, 2023

The resistance of microorganisms to antimicrobials has endangered the health many people across world. Overcoming problem will require invention molecules with a new mechanism action so that no cross-resistance existing therapies occurs. Because their powerful antibacterial activity against wide spectrum Gram-positive and Gram-negative bacterial strains, heterocyclic compounds are appealing candidates for medicinal chemists. In this regard, as unique hybrid compounds, we synthesized novel family bis-thiazoles linked quinoxaline or thienothiophene via 2-phenoxy-N-arylacetamide moiety. target were by reacting relevant bis(α-haloketones) corresponding thiosemicarbazones in EtOH at reflux few drops TEA. Under comparable reaction conditions, isomeric bis(thiazoles) appropriate bis(thiosemicarbazone) respective α-haloketones. structures confirmed using elements spectral data. All tested vitro. With an inhibitory zone width 12 mm, compound 12a had same reference medication tobramycin Staphylococcus aureus. Compound 12b showed 20 mg/mL minimum concentration (MIC) Bacillus subtilis. Some molecular docking two proteins (dihydrofolate reductase tyrosyl-tRNA synthetase).

Language: Английский

Citations

6

Design, synthesis, molecular docking, ADMET studies, and biological activity evaluation of new 2-({[3-aryl-1,2,4-oxadiazol-5-yl)methyl]thio}-1H-benzimidazoles and 6-amino-6-aryl-5,6-dihydro[1,6,2,4]oxathiadiazocino[4,5-a]benzimidazol-3(2H)-ones DOI
Mohamed H. Sharaf, Amr H. Moustafa,

Rami J. Obaid

et al.

Journal of Molecular Structure, Journal Year: 2023, Volume and Issue: 1295, P. 136708 - 136708

Published: Sept. 29, 2023

Language: Английский

Citations

4

Interaction of Thiophene and Their Derivatives with BRCA-1 Using a Theoretical Model DOI
Lauro Figueroa-Valverde, Rosas‐Nexticapa Marcela, Magdalena Alvarez-Ramirez

et al.

Clinical Cancer Investigation Journal, Journal Year: 2024, Volume and Issue: 13(2), P. 40 - 44

Published: Jan. 1, 2024

Language: Английский

Citations

1

Recruitment of hexahydroquinoline as anticancer scaffold targeting inhibition of wild and mutants EGFR (EGFR WT , EGFR T790M , and EGFR L858R ) DOI Creative Commons

Mahmoud G. Abo Al-Hamd,

Haytham O. Tawfik, Omeima Abdullah

et al.

Journal of Enzyme Inhibition and Medicinal Chemistry, Journal Year: 2023, Volume and Issue: 38(1)

Published: Aug. 7, 2023

Hexahydroquinoline (HHQ) scaffold was constructed and recruited for development of new series anticancer agents. Thirty-two compounds were synthesised where x-ray crystallography performed to confirm enantiomerism. Thirteen showed moderate good activity against NCI 60 cancer cell lines, with GI % mean up 74%

Language: Английский

Citations

3

Ferula ferulaeoides ethyl acetate extract induces apoptosis in esophageal cancer cells via mitochondrial and PI3K/Akt/Bad pathways DOI Creative Commons

Yerlan Bahetjan,

Wenqi Liu,

Muguli Muhaxi

et al.

Arabian Journal of Chemistry, Journal Year: 2023, Volume and Issue: 16(12), P. 105291 - 105291

Published: Sept. 26, 2023

Ferula ferulaeoides (Steud.) Korovin is a traditional ethnopharmacological plant used for lump elimination and as spice, especially in places like India. It has also been employed the livestock food industries. This investigation aimed to explore anti-tumor mechanisms of ethyl acetate extract fractions dried roots (FF-EtOAc) on esophageal cancer (EC) cells. Furthermore, it was hypothesized that FF-EtOAc could inhibit EC cells growths by inducing apoptosis. In time- dose-dependent manner, considerably reduced number migrating And inhibited growth vivo, less toxic nude mice. terms anticancer mechanism, findings revealed activating mitochondrial signaling pathways PI3K/Akt/Bad pathways. Through both vitro vivo experiments, significantly exhibited anti-esophageal activity. The anti-EC activity may be due activation apoptotic

Language: Английский

Citations

2

New S- and N-alkyl functionalized bis-1,2,4-Triazolyl-based Derivatives as Potential Dual EGFRWT and EGFRT790M Inhibitors: Synthesis, Anti-proliferative Evaluation, Molecular Docking Study and ADMET Studies DOI

A. M. I. Ahmed,

Moustafa O. Aboelez,

Hend A. A. Ezelarab

et al.

Journal of Molecular Structure, Journal Year: 2024, Volume and Issue: unknown, P. 140720 - 140720

Published: Nov. 1, 2024

Language: Английский

Citations

0