Cover Image

Synthesis, biological evaluation, and molecular docking of new series of antitumor and apoptosis inducers designed as VEGFR-2 inhibitors

Based on quinazoline, quinoxaline, and nitrobenzene scaffolds and on pharmacophoric features of VEGFR-2 inhibitors, 17 novel compounds were designed and synthesised. VEGFR-2 IC50 values ranged from 60.00 to 123.85 nM for the new derivatives compared to 54.00 nM for sorafenib. Compounds 15a, 15b, and...

Full description

Saved in:

Bibliographic Details
Main Authors:	Abdallah E. Abdallah (Author), Reda R. Mabrouk (Author), Maged Mohammed Saleh Al Ward (Author), Sally I. Eissa (Author), Eslam B. Elkaeed (Author), Ahmed B. M. Mehany (Author), Mariam A. Abo-Saif (Author), Ola A. El-Feky (Author), Mohamed S. Alesawy (Author), Mohamed Ayman El-Zahabi (Author)
Format:	Book
Published:	Taylor & Francis Group, 2022-12-01T00:00:00Z.
Subjects:	article
Online Access:	Connect to this object online.
Tags:	Add Tag No Tags, Be the first to tag this record!

Similar Items

New quinoline and isatin derivatives as apoptotic VEGFR-2 inhibitors: design, synthesis, anti-proliferative activity, docking, ADMET, toxicity, and MD simulation studies
by: Eslam B. Elkaeed, et al.
Published: (2022)

New Series of VEGFR-2 Inhibitors and Apoptosis Enhancers: Design, Synthesis and Biological Evaluation
by: Abdallah AE, et al.
Published: (2022)

Anti-cancer and immunomodulatory evaluation of new nicotinamide derivatives as potential VEGFR-2 inhibitors and apoptosis inducers: in vitro and in silico studies
by: Reda G. Yousef, et al.
Published: (2022)

Design and synthesis of thiazolidine-2,4-diones hybrids with 1,2-dihydroquinolones and 2-oxindoles as potential VEGFR-2 inhibitors: in-vitro anticancer evaluation and in-silico studies
by: Mohammed S. Taghour, et al.
Published: (2022)

Discovery of new nicotinamides as apoptotic VEGFR-2 inhibitors: virtual screening, synthesis, anti-proliferative, immunomodulatory, ADMET, toxicity, and molecular dynamic simulation studies
by: Reda G. Yousef, et al.
Published: (2022)

Discovery of new quinolines as potent colchicine binding site inhibitors: design, synthesis, docking studies, and anti-proliferative evaluation
by: Mohamed Hagras, et al.
Published: (2021)

Computer-assisted drug discovery (CADD) of an anti-cancer derivative of the theobromine alkaloid inhibiting VEGFR-2
by: Ibrahim H. Eissa, et al.
Published: (2023)

1,3,4-Oxadiazole-naphthalene hybrids as potential VEGFR-2 inhibitors: design, synthesis, antiproliferative activity, apoptotic effect, and in silico studies
by: Mohamed Hagras, et al.
Published: (2022)

New benzoxazole derivatives as potential VEGFR-2 inhibitors and apoptosis inducers: design, synthesis, anti-proliferative evaluation, flowcytometric analysis, and in silico studies
by: Hazem Elkady, et al.
Published: (2022)

Benzoxazole derivatives as new VEGFR-2 inhibitors and apoptosis inducers: design, synthesis, in silico studies, and antiproliferative evaluation
by: Mohammed S. Taghour, et al.
Published: (2022)

Discovery of novel thiazolyl-pyrazolines as dual EGFR and VEGFR-2 inhibitors endowed with in vitro antitumor activity towards non-small lung cancer
by: Esraa A. Abdelsalam, et al.
Published: (2022)

Novel N-Arylmethyl-aniline/chalcone hybrids as potential VEGFR inhibitors: synthesis, biological evaluations, and molecular dynamic simulations
by: Hesham Haffez, et al.
Published: (2023)

Topo II inhibition and DNA intercalation by new phthalazine-based derivatives as potent anticancer agents: design, synthesis, anti-proliferative, docking, and in vivo studies
by: Mohamed M. Khalifa, et al.
Published: (2022)

Discovery of sulfonamide-tethered isatin derivatives as novel anticancer agents and VEGFR-2 inhibitors
by: Moataz A. Shaldam, et al.
Published: (2023)

Design, Molecular Docking, Synthesis, Anticancer and Anti-Hyperglycemic Assessments of Thiazolidine-2,4-diones Bearing Sulfonylthiourea Moieties as Potent VEGFR-2 Inhibitors and PPARγ Agonists
by: Mohamed A. Abdelgawad, et al.
Published: (2022)

Antiangiogenic and Antitumoral Effects Mediated by a Vascular Endothelial Growth Factor Receptor 1 (VEGFR-1)-Targeted DNAzyme
by: Liangfang Shen, et al.
Published: (2013)

Synthesis, antitumor activity, and molecular docking study of 2-cyclopentyloxyanisole derivatives: mechanistic study of enzyme inhibition
by: Walaa M. El-Husseiny, et al.
Published: (2020)

Pomegranate peel extract protects against the development of diabetic cardiomyopathy in rats by inhibiting pyroptosis and downregulating LncRNA-MALAT1
by: Mariam Ali Abo-Saif, et al.
Published: (2023)

Discovery of new 1H-pyrazolo[3,4-d]pyrimidine derivatives as anticancer agents targeting EGFRWT and EGFRT790M
by: Ahmed A. Gaber, et al.
Published: (2022)

Improving the Antitumor Activity and Bioavailability of Sonidegib for the Treatment of Skin Cancer
by: Amr Gamal, et al.
Published: (2021)

Design, synthesis, docking, ADMET studies, and anticancer evaluation of new 3-methylquinoxaline derivatives as VEGFR-2 inhibitors and apoptosis inducers
by: Mohammed M. Alanazi, et al.
Published: (2021)

Prevalence of migraine, its effect, and some comorbid psychiatric disorders among female medical students at Al-Azhar University in Cairo
by: Eman Saif, et al.
Published: (2017)

Correlation between pulp sensibility and magnetic resonance signal intensity following regenerative endodontic procedures in mature necrotic teeth- a retrospective cohort study
by: Noha Mohamed El-Kateb, et al.
Published: (2024)

Design, synthesis, and anti-cancer evaluation of new pyrido[2,3-d]pyrimidin-4(3H)-one derivatives as potential EGFRWT and EGFRT790M inhibitors and apoptosis inducers
by: Heba S. A. Elzahabi, et al.
Published: (2022)

Novel piperazine-chalcone hybrids and related pyrazoline analogues targeting VEGFR-2 kinase; design, synthesis, molecular docking studies, and anticancer evaluation
by: Marwa F. Ahmed, et al.
Published: (2021)

Development of 3-methyl/3-(morpholinomethyl)benzofuran derivatives as novel antitumor agents towards non-small cell lung cancer cells
by: Mohammad M. Al-Sanea, et al.
Published: (2021)

Design, synthesis, docking, MD simulations, and anti-proliferative evaluation of thieno[2,3-d]pyrimidine derivatives as new EGFR inhibitors
by: Eman A. Sobh, et al.
Published: (2023)

Mechanism Underlying Triple VEGFR Inhibitor Tivozanib-Induced Hypertension in Mice Model
by: Wael A. Alanazi, et al.
Published: (2023)

Impact of different CAD/CAM materials on internal and marginal adaptations and fracture resistance of endocrown restorations with: 3D finite element analysis
by: Shaimaa Ahmed Abo El-Farag, et al.
Published: (2023)

New benzothiazole hybrids as potential VEGFR-2 inhibitors: design, synthesis, anticancer evaluation, and in silico study
by: Mohammad M. Al-Sanea, et al.
Published: (2023)

Design, Synthesis, Molecular Modeling, and Anticancer Evaluation of New VEGFR-2 Inhibitors Based on the Indolin-2-One Scaffold
by: Mohamed A. Abdelgawad, et al.
Published: (2022)

The Impact of Armed Conflict on the Prevalence and Transmission Dynamics of HIV Infection in Libya
by: Mohamed Ali Daw, et al.
Published: (2022)

The antitumor effect of tanshinone IIA on anti-proliferation and decreasing VEGF/VEGFR2 expression on the human non-small cell lung cancer A549 cell line
by: Jun Xie, et al.
Published: (2015)

Design, Synthesis, Pharmacological Evaluation of Quinazolin-4(3H)-Ones Bearing Urea Functionality as Potential VEGFR-2 Inhibitors
by: Al-Sanea MM, et al.
Published: (2024)

Immunohistochemical study of VEGF-A, VEGFR-1, VEGFR-2 and CD34 expression in сolorectal adenocarcinoma progression
by: M. A. Shyshkin
Published: (2019)

Thrombus-in-transit: Simple solution for a complex situation
by: Ahmed Mohsen, et al.
Published: (2021)

A bivalent cyclic RGD-siRNA conjugate enhances the antitumor effect of apatinib via co-inhibiting VEGFR2 in non-small cell lung cancer xenografts
by: Lumin Liao, et al.
Published: (2021)

Vascular endothelial growth factor and its soluble receptors VEGFR-1 and VEGFR-2 in the serum of patients with systemic lupus erythematosus
by: Ewa Robak, et al.
Published: (2003)

The Effect of Encapsulated Apigenin Nanoparticles on HePG-2 Cells through Regulation of P53
by: Mayada Mohamed Mabrouk Zayed, et al.
Published: (2022)

Design, synthesis, and apoptotic antiproliferative action of new 1,2,3-triazole/1,2,4-oxadiazole hybrids as dual EGFR/VEGFR-2 inhibitors
by: Mohamed A. Mahmoud, et al.
Published: (2024)