Phthalazine Derivatives as VEGFR‐2 Inhibitors: Docking, ADMET, Synthesis, Design, Anticancer Evaluations, and Apoptosis Inducers DOI Open Access

Hatem Hussein Bayoumi,

Mohamed‐Kamal Ibrahim,

Mohammed A. Dahab

et al.

Drug Development Research, Journal Year: 2024, Volume and Issue: 86(1)

Published: Dec. 24, 2024

New phthalazine-derived inhibitors for VEGFR-2 were synthesized anticancer evaluations. Also, docking studies performed to explore the suggested binding orientations of novel derivatives inside site VEGFR-2. The achieved biological data extremely interrelated that study. In specific, derivative 3f was greatest effective compound against HepG2 and MCF-7 cancer cell lines with IC

Language: Английский

Anticancer evaluations of iodoquinazoline substituted with allyl and/or benzyl as dual inhibitors of EGFRWT and EGFRT790M: design, synthesis, ADMET and molecular docking DOI Creative Commons
Ahmed K. B. Aljohani, Khaled El‐Adl, Basmah Almohaywi

et al.

RSC Advances, Journal Year: 2024, Volume and Issue: 14(12), P. 7964 - 7980

Published: Jan. 1, 2024

Fifteen new iodoquinazoline derivatives, 5a,b to 18, are reported in this study and their anticancer evaluation as dual inhibitors of EGFR WT T790M .

Language: Английский

Citations

5
Exploration of the VEGFR-2 inhibition activity of phthalazine derivatives: design, synthesis, cytotoxicity, ADMET, molecular docking and dynamic simulation DOI Creative Commons

Hatem Hussein Bayoumi,

Mohamed‐Kamal Ibrahim,

Mohammed A. Dahab

et al.

RSC Advances, Journal Year: 2024, Volume and Issue: 14(30), P. 21668 - 21681

Published: Jan. 1, 2024

Novel phthalazine derivatives were designed, synthesized and evaluated against Hep G2 MCF-7 as VEGFR-2 inhibitors.

Language: Английский

Citations

4
Discovery of 1-phenyl-1,2,3-triazole ureas as dual VEGFR-2/JNK-1 type II kinase inhibitors targeting pancreatic cancer DOI
Wagdy M. Eldehna, Eslam Roshdy,

Maha-Hamadien Abdulla

et al.

International Journal of Biological Macromolecules, Journal Year: 2025, Volume and Issue: unknown, P. 142372 - 142372

Published: March 1, 2025

Language: Английский

Citations

0
EGFR Inhibitors Across Generations: Progress, Challenges, and Future Directions DOI

Vishal G. Deshmukh,

Suryakant B. Sapkal,

Suchita S. Gadekar

et al.

Journal of Molecular Structure, Journal Year: 2025, Volume and Issue: unknown, P. 142326 - 142326

Published: April 1, 2025

Language: Английский

Citations

0
New benzimidazole‐oxadiazole derivatives as potent VEGFR‐2 inhibitors: Synthesis, anticancer evaluation, and docking study DOI Creative Commons
Ulviye Acar Çevik, İsmail Çeli̇k, Şennur Görgülü

et al.

Drug Development Research, Journal Year: 2024, Volume and Issue: 85(4)

Published: June 1, 2024

Abstract We report herein, the design and synthesis of benzimidazole‐oxadiazole derivatives as new inhibitors for vascular endothelial growth factor receptor‐2 (VEGFR‐2). The designed members were assessed their in vitro anticancer activity against three cancer cell lines two normal lines; A549, MCF‐7, PANC‐1, hTERT‐HPNE CCD‐19Lu. Compounds 4c 4d found to be most effective compounds lines. then tested VEGFR‐2 inhibitory activity, safety profiles, selectivity indices using CCD‐19Lu It was determined that compound safe member produced chemical family. Vascular A (VEGFA) immunolocalizations evaluated relative control by VEGFA immunofluorescence staining. inhibited enzyme with half‐maximal concentration values 0.475 ± 0.021 0.618 0.028 µM, respectively. Molecular docking target carried out active site (Protein Data Bank: 4ASD).

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
Rationale, in silico docking, ADMET profile, design, synthesis and cytotoxicity evaluations of phthalazine derivatives as VEGFR-2 inhibitors and apoptosis inducers DOI Creative Commons

Hatem Hussein Bayoumi,

Mohamed‐Kamal Ibrahim,

Mohammed A. Dahab

et al.

RSC Advances, Journal Year: 2024, Volume and Issue: 14(37), P. 27110 - 27121

Published: Jan. 1, 2024

New phthalazine derivatives as vascular endothelial growth factor receptor-2 (VEGFR-2) inhibitors were synthesized joined to different spacers including pyrazole, α,β-unsaturated ketonic fragment, pyrimidinone and/or pyrimidinthione.

Language: Английский

Citations

2
Exploration of cytotoxicity of iodoquinazoline derivatives as inhibitors of both VEGFR‐2 and EGFRT790M: Molecular docking, ADMET, design, and syntheses DOI Open Access
Marwa Alsulaimany,

Sanadelaslam S. A. El‐Hddad,

Zuhir S. M. Akrim

et al.

Archiv der Pharmazie, Journal Year: 2024, Volume and Issue: 357(11)

Published: Aug. 1, 2024

Novel inhibitors of epidermal growth factor receptor (EGFR)

Language: Английский

Citations

1
Phthalazine Derivatives as VEGFR‐2 Inhibitors: Docking, ADMET, Synthesis, Design, Anticancer Evaluations, and Apoptosis Inducers DOI Open Access

Hatem Hussein Bayoumi,

Mohamed‐Kamal Ibrahim,

Mohammed A. Dahab

et al.

Drug Development Research, Journal Year: 2024, Volume and Issue: 86(1)

Published: Dec. 24, 2024

New phthalazine-derived inhibitors for VEGFR-2 were synthesized anticancer evaluations. Also, docking studies performed to explore the suggested binding orientations of novel derivatives inside site VEGFR-2. The achieved biological data extremely interrelated that study. In specific, derivative 3f was greatest effective compound against HepG2 and MCF-7 cancer cell lines with IC

Language: Английский

Citations

0