Advances in structural identification of some thieno[2,3-d]pyrimidine scaffolds as antitumor molecules: Synthetic approaches and control programmed cancer cell death potential DOI

Aml E.-S. Mghwary,

Rasha A. Hassan,

Peter A. Halim

et al.

Bioorganic Chemistry, Journal Year: 2024, Volume and Issue: 154, P. 107985 - 107985

Published: Nov. 27, 2024

Language: Английский

Identification of indole-grafted pyrazolopyrimidine and pyrazolopyridine derivatives as new anti-cancer agents: Synthesis, biological assessments, and molecular modeling insights DOI
Wagdy M. Eldehna, Haytham O. Tawfik,

Maha-Hamadien Abdulla

et al.

Bioorganic Chemistry, Journal Year: 2024, Volume and Issue: 153, P. 107804 - 107804

Published: Sept. 6, 2024

Language: Английский

Citations

6
EGFR as therapeutic target to develop new generation tyrosine kinase inhibitors against breast cancer: A critical review DOI Creative Commons
Ruby Mariam Raju,

Jeffin Joy A,

Raghavendra Nulgumnalli Manjunathaiah

et al.

Results in Chemistry, Journal Year: 2024, Volume and Issue: 7, P. 101490 - 101490

Published: Jan. 1, 2024

Epidermal Growth Factor Receptor is a multifunctional receptor and an important member of tyrosine kinase family. Investigation on mechanism tumour progression its suppression has identified prominent role EGFR, which was the first amongst EGFR various cellular functions but aberration results in development. About half breast cancer cases overexpresses making it as appropriate target for discovery molecular based targeted therapeutics i.e., inhibitors. This review focusses structural features, signaling pathways cancer. In addition to this, recent developments TKIs targeting are discussed along with activity relationships. Also, article highlights inhibitors that under clinical study patents.

Language: Английский

Citations

5
Muti-target rationale design of novel substituted N-phenyl-2-((6-phenylpyridazin-3-yl)thio)acetamide candidates as telomerase/JAK1/STAT3/TLR4 inhibitors: In vitro and in vivo investigations DOI
Moataz A. Shaldam, Mai H. A. Mousa, Haytham O. Tawfik

et al.

Bioorganic Chemistry, Journal Year: 2024, Volume and Issue: 153, P. 107843 - 107843

Published: Sept. 24, 2024

Language: Английский

Citations

5
Tailored horseshoe-shaped nicotinonitrile scaffold as dual promising c-Met and Pim-1 inhibitors: Design, synthesis, SAR and in silico study DOI
Samy Mohamady, Ahmed Khalil, Bassem H. Naguib

et al.

Bioorganic Chemistry, Journal Year: 2023, Volume and Issue: 143, P. 106988 - 106988

Published: Nov. 20, 2023

Language: Английский

Citations

9
A decade's overview of 2‐aminothiophenes and their fused analogs as promising anticancer agents DOI

Donia G. Darwish,

Hany A.M. El-Sherief, Salah A. Abdel‐Aziz

et al.

Archiv der Pharmazie, Journal Year: 2024, Volume and Issue: 357(6)

Published: March 5, 2024

Abstract Over the past decades, cancer has been a challenging domain for medicinal chemists as it is an international health concern. In association, small molecules such 2‐aminothiophenes and their derivatives showed significant antitumor activity through variable modes of action. Therefore, this article aims to review advances regarding these core scaffolds over 10 years, where fused analogs are classified discussed according biological mode action, in interest boosting new design pathways develop targeted candidates.

Language: Английский

Citations

3
DFT and molecular simulation validation of the binding activity of PDEδ inhibitors for repression of oncogenic k-Ras DOI Creative Commons
Taghreed A. Majrashi, Ahmed Sabt, Hadia Almahli

et al.

PLoS ONE, Journal Year: 2024, Volume and Issue: 19(3), P. e0300035 - e0300035

Published: March 8, 2024

The development of effective drugs targeting the K-Ras oncogene product is a significant focus in anticancer drug development. Despite lack successful Ras signaling inhibitors, recent research has identified PDEδ, KRAS transporter, as potential target for inhibiting oncogenic pathway. This study aims to investigate interactions between eight inhibitors (deltarazine, deltaflexin 1 and 2, its analogues) PDEδ understand their binding modes. will utilize computational techniques such density functional theory (DFT) molecular electrostatic surface (MESP), docking, site analyses, dynamic (MD) simulations, electronic structure computations, predictions free energy. Molecular simulations be used predict conformations pharmacophoric features active examined structures. energies determined using MMPB(GB)SA method compared with observed potency values tested compounds. approach enhance understanding selective mechanism, which could contribute novel signaling.

Language: Английский

Citations

3
Discovery of new quinoline derivatives bearing 1-aryl-1,2,3-triazole motif as influenza H1N1 virus neuraminidase inhibitors DOI
Ahmed Sabt, Eman F. Khaleel, Moataz A. Shaldam

et al.

Bioorganic Chemistry, Journal Year: 2024, Volume and Issue: 151, P. 107703 - 107703

Published: Aug. 6, 2024

Language: Английский

Citations

3
Advances in Cancer Therapy: A Comprehensive Review of CDK and EGFR Inhibitors DOI Creative Commons
Mohammed Hawash

Cells, Journal Year: 2024, Volume and Issue: 13(19), P. 1656 - 1656

Published: Oct. 6, 2024

Protein kinases have essential responsibilities in controlling several cellular processes, and their abnormal regulation is strongly related to the development of cancer. The implementation protein kinase inhibitors has significantly transformed cancer therapy by modifying treatment strategies. These received substantial FDA clearance recent decades. emerged as primary objectives for therapeutic interventions, particularly context treatment. At present, 69 therapeutics been approved that target approximately 24 kinases, which are specifically prescribed neoplastic illnesses. novel agents inhibit certain such receptor protein-tyrosine protein-serine/threonine dual-specificity nonreceptor kinases. This review presents a comprehensive overview targets inhibitors, with specific focus on cyclin-dependent (CDKs) epidermal growth factor (EGFR). majority reviewed studies commenced an assessment cell lines concluded biological evaluation individual targets. articles provide detailed information structural features potent anticancer activity, refers ability selectively cancer-promoting including CDKs EGFR. Additionally, latest FDA-approved targeting these enzymes were highlighted accordingly.

Language: Английский

Citations

3
Discovery of new 1,3-diphenylurea appended aryl pyridine derivatives as apoptosis inducers through c-MET and VEGFR-2 inhibition: design, synthesis, in vivo and in silico studies DOI

Heba A. Elsebaie,

Mohamed S. Nafie, Haytham O. Tawfik

et al.

RSC Medicinal Chemistry, Journal Year: 2024, Volume and Issue: 15(7), P. 2553 - 2569

Published: Jan. 1, 2024

A new 1,3-diphenylurea appended aryl pyridine derivative was designed, synthesized and characterized as c-MET VEGFR-2 inhibitors to induce apoptosis against MCF-7 cells.

Language: Английский

Citations

1
Synthesis, enzyme inhibition assay, and molecular modeling study of novel pyrazolines linked to 4-methylsulfonylphenyl scaffold: antitumor activity and cell cycle analysis DOI Creative Commons
Alaa A.‐M. Abdel‐Aziz, Adel S. El‐Azab, Simone Brogi

et al.

RSC Advances, Journal Year: 2024, Volume and Issue: 14(31), P. 22132 - 22146

Published: Jan. 1, 2024

Antitumor activity using 59 cancer cell lines and enzyme inhibitory of a newly synthesized pyrazoline-linked 4-methylsulfonylphenyl scaffold (compounds 18a–q) were measured compared with those standard drugs.

Language: Английский

Citations

1