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

Discovery of Novel Pyridazine-Tethered Sulfonamides as Carbonic Anhydrase II Inhibitors for the Management of Glaucoma DOI
Haytham O. Tawfik, Mohamed M. Saleh, Andrea Ammara

et al.

Journal of Medicinal Chemistry, Journal Year: 2024, Volume and Issue: 67(2), P. 1611 - 1623

Published: Jan. 11, 2024

As a progressive neuropathic condition, glaucoma can cause lifelong blindness if left untreated. Novel phenylpyridazine-tethered sulfonamides were designed as selective inhibitors for carbonic anhydrase (CA) isoform II to find effective therapeutic agents glaucoma. Subsequently, the target synthesized and assessed their inhibitory action against cytosolic CA I II. Interestingly, molecules poorly inhibited while exhibiting low subnanomolar potency Compound

Language: Английский

Citations

16
Development of new thieno[2,3-d]pyrimidines as dual EGFR and STAT3 inhibitors endowed with anticancer and pro-apoptotic activities DOI

Heba A. Elsebaie,

Tarek F. El‐Moselhy, Eman A. El-Bastawissy

et al.

Bioorganic Chemistry, Journal Year: 2024, Volume and Issue: 143, P. 107101 - 107101

Published: Jan. 4, 2024

Language: Английский

Citations

15
Discovery and Mechanistic Studies of Dual-Target Hits for Carbonic Anhydrase IX and VEGFR-2 as Potential Agents for Solid Tumors: X-ray, In Vitro, In Vivo, and In Silico Investigations of Coumarin-Based Thiazoles DOI
Salma M. Hefny, Tarek F. El‐Moselhy,

Nabaweya Sharaf El-Din

et al.

Journal of Medicinal Chemistry, Journal Year: 2024, Volume and Issue: 67(9), P. 7406 - 7430

Published: April 20, 2024

A dual-targeting approach is predicted to yield better cancer therapy outcomes. Consequently, a series of coumarin-based thiazoles (5a–h, 6, and 7a–e) were designed constructed as potential carbonic anhydrase (CA) VEGFR-2 suppressors. The inhibitory actions the target compounds assessed against CA isoforms IX VEGFR-2. assay results showed that 5a, 5d, 5e can effectively inhibit both targets. cytotoxic effects tested on pancreatic, breast, prostate cells (PANC1, MCF7, PC3). Further mechanistic investigation disclosed ability interrupt PANC1 cell progression in S stage by triggering apoptotic cascade, seen increased levels caspases 3, 9, BAX, alongside Bcl-2 decline. Moreover, vivo efficacy compound an antitumor agent was evaluated. Also, molecular docking dynamics displayed distinctive interactions between binding pockets.

Language: Английский

Citations

15
A new framework for novel analogues of pazopanib as potent and selective human carbonic anhydrase inhibitors: Design, repurposing rational, synthesis, crystallographic, in vivo and in vitro biological assessments DOI
Salma M. Hefny, Tarek F. El‐Moselhy,

Nabaweya Sharaf El-Din

et al.

European Journal of Medicinal Chemistry, Journal Year: 2024, Volume and Issue: 274, P. 116527 - 116527

Published: May 24, 2024

Language: Английский

Citations

12
Novel imidazo[2,1-b]thiazoles and imidazo[1,2-a]pyridines tethered with indolinone motif as VEGFR-2 inhibitors and apoptotic inducers: Design, synthesis and biological evaluations DOI
Mahmoud S. Elkotamy, Mohamed K. Elgohary, Sara T. Al‐Rashood

et al.

Bioorganic Chemistry, Journal Year: 2024, Volume and Issue: 151, P. 107644 - 107644

Published: July 15, 2024

Language: Английский

Citations

12
Novel sulfonamide-tethered Schiff bases as anti-proliferative agents with VEGFR-2 inhibitory activity: Synthesis, biological assessment, and molecular dynamic simulations DOI
Moataz A. Shaldam,

Maha-Hamadien Abdulla,

Andrea Angeli

et al.

Journal of Molecular Structure, Journal Year: 2024, Volume and Issue: 1309, P. 138148 - 138148

Published: March 26, 2024

Language: Английский

Citations

8
Unveiling the potential of isatin-grafted phenyl-1,2,3-triazole derivatives as dual VEGFR-2/STAT-3 inhibitors: Design, synthesis and biological assessments DOI

Heba A. Elsebaie,

Maha-Hamadien Abdulla,

Zainab M. Elsayed

et al.

Bioorganic Chemistry, Journal Year: 2024, Volume and Issue: 151, P. 107626 - 107626

Published: July 10, 2024

Language: Английский

Citations

8
Design, synthesis, molecular docking and dynamic studies of novel thienopyrimidine analogs linked to 1,2,3-triazole-bearing acetamide derivatives as anti-oxidant agents DOI

Tammineni Lalita Kumari,

Alice R. Robert, Prashantha Karunakar

et al.

Journal of Molecular Structure, Journal Year: 2024, Volume and Issue: 1307, P. 137883 - 137883

Published: Feb. 29, 2024

Language: Английский

Citations

6
Synthesis and biological evaluation of 1-phenyl-tetrahydro-β-carboline-based first dual PRMT5/EGFR inhibitors as potential anticancer agents DOI
Juan Zhang, Xuliang Liu,

Na Sa

et al.

European Journal of Medicinal Chemistry, Journal Year: 2024, Volume and Issue: 269, P. 116341 - 116341

Published: March 18, 2024

Language: Английский

Citations

6
Discovery of new sulfonamide-tethered 2-aryl-4-anilinoquinazolines as the first-in-class dual carbonic anhydrase and EGFR inhibitors DOI
Wagdy M. Eldehna,

Zainab M. Elsayed,

Andrea Ammara

et al.

International Journal of Biological Macromolecules, Journal Year: 2024, Volume and Issue: 279, P. 135010 - 135010

Published: Aug. 26, 2024

Language: Английский

Citations

6