Design and Discovery of New Dual Carbonic Anhydrase IX and VEGFR‐2 Inhibitors Based on the Benzenesulfonamide‐Bearing 4‐Thiazolidinones/2,4‐Thiazolidinediones Scaffold DOI Open Access
Merve Zengin, Oya Ünsal Tan, Suna Sabuncuoğlu

et al.

Drug Development Research, Journal Year: 2024, Volume and Issue: 85(8)

Published: Dec. 1, 2024

Dual-targeting drug design has become a popular approach in investigating and developing potent anticancer agents. In this regard, carbonic anhydrase (CAIX) vascular endothelial growth factor receptor (VEGFR-2) are emerging as highly effective targets the battle against cancer. present study, two series of 4-thiazolidinones/2,4-thiazolidinediones carrying 2-methylbenzenesulfonamide derivatives were designed synthesized potential dual CAIX/VEGFR-2 inhibitors. All target compounds evaluated CAIX enzyme compared to dorzolamide acetazolamide, subsequently most inhibitors (3a, 3b, 3o, 6d, 6g, 6i) selected evaluate their inhibitory activity VEGFR-2 using sorafenib reference drug. These also MCF-7 breast cancer cells murine fibroblast 3T3 cell line. According results, 3b (CAIX IC

Language: Английский

Unveiling the Therapeutic Potential of Quinazolinone Derivatives in Cancer Treatment: A Comprehensive Exploration DOI
Jasneet Kaur,

Sukhmeet Kaur,

Muskan

et al.

ChemistrySelect, Journal Year: 2024, Volume and Issue: 9(32)

Published: Aug. 22, 2024

Abstract Quinazolinone derivatives have garnered attention for their diverse biological activities, including anticancer properties. This review combines findings from 2018 to 2024, focusing on the impact of quinazolinones cancer cells, tubulin formation, and EGFR/PI3 K pathways. By unraveling intricacies structure‐activity relationships, this endeavors provide guidance researchers in identifying promising avenues development treatments. Although vitro studies underscore significant potential, it is imperative that future research prioritizes pre‐clinical investigations seamlessly traverse transitional phase towards clinical applications, thereby propelling advancement quinazolinone‐based therapy.

Language: Английский

Citations

3
Novel quinazolin-4-one based derivatives bearing 1,2,3-triazole and glycoside moieties as potential cytotoxic agents through dual EGFR and VEGFR-2 inhibitory activity DOI Creative Commons
Adel A.‐H. Abdel‐Rahman, Mohamed N. El-Bayaa,

Asmaa Sobhy

et al.

Scientific Reports, Journal Year: 2024, Volume and Issue: 14(1)

Published: Oct. 23, 2024

The toxicity that was caused by the developed medications for anticancer treatment is, unfortunately, an earnest problem stemming from various involved targets, and accordingly, intense research overcoming such a phenomenon remains indispensable. In current inquiry, innovative category of substituted quinazoline-based glycosides incorporating core 1,2,3-triazole attached to distinct acetylated likewise deprotected sugar segments are created produced synthetically. resulted 1,2,3-triazolyl-glycosides products were investigated their ability cause cytotoxicity several human cancer cell lines. quinazoline based glycosyl-1,2,3-triazoles 10-13 with free hydroxy moiety revealed excellent potency against (IC

Language: Английский

Citations

3
Design, synthesis, docking, ADMET and anticancer evaluations of N-alkyl substituted iodoquinazoline derivatives as dual VEGFR-2 and EGFR inhibitors DOI Creative Commons
Marwa Alsulaimany, Khaled El‐Adl, Ahmed K. B. Aljohani

et al.

RSC Advances, Journal Year: 2023, Volume and Issue: 13(51), P. 36301 - 36321

Published: Jan. 1, 2023

Fifteen new 1-alkyl-6-iodoquinazoline derivatives 5a–d to 9a–e were designed and synthesized their anticancer activities evaluated against HepG2, MCF-7, HCT116 A549 cancer cell lines via dual targeting of EGFR VEGFR-2.

Language: Английский

Citations

7
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
Design, Synthesis, and Biological Evaluation of Novel Quinazoline Derivatives Possessing a Trifluoromethyl Moiety as Potential Antitumor Agents DOI

M Chen,

Sha Cheng,

Xing Dai

et al.

Chemistry & Biodiversity, Journal Year: 2024, Volume and Issue: 21(5)

Published: April 11, 2024

Abstract A novel series of trifluoromethyl‐containing quinazoline derivatives with a variety functional groups was designed, synthesized, and tested for their antitumor activity by following pharmacophore hybridization strategy. Most the 20 compounds displayed moderate to excellent antiproliferative against five different cell lines (PC3, LNCaP, K562, HeLa, A549). After three rounds screening structural optimization, compound 10 b identified as most potent one, IC 50 values 3.02, 3.45, 3.98 μM PC3, K562 cells, respectively, which were comparable effect positive control gefitinib. To further explore mechanism action cancer, experiments focusing on apoptosis induction, cycle arrest, migration assay conducted. The results showed that able induce prevent tumor migration, but had no cells.

Language: Английский

Citations

1
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
Sulfonyl-acetohydrazide derivatives as juvenile hormone mimics to be insect growth regulators DOI
Neetika Kumari, Manisha Chaudhary, Pamita Awasthi

et al.

Bioorganic Chemistry, Journal Year: 2024, Volume and Issue: 153, P. 107781 - 107781

Published: Sept. 5, 2024

Language: Английский

Citations

1
Halogen‐based quinazolin‐4(3H)‐one derivatives as MCF‐7 breast cancer inhibitors: Current developments and structure–activity relationship DOI

Rachana Upadhyay,

P. K. Tandel,

Amit B. Patel

et al.

Archiv der Pharmazie, Journal Year: 2024, Volume and Issue: 358(1)

Published: Nov. 13, 2024

Abstract Currently, cancer is a serious health challenge with predominance beyond restrictions. Breast remains one of the major contributors to cancer‐related morbidity and mortality in women. Chemotherapy continues be crucial treatment all variants cancer. Several antitumor drugs are presently different phases clinical trials, whereas many more have been approved for use. However, these potential cause adverse effects, certain individuals may become resistant them, which would eventually reduce drug's efficacy. Therefore, it essential discover, develop, improve newer anticancer drug molecules that could potentially inhibit proliferative pathways. In recent years, quinazolinone derivatives, specifically halogen‐substituted 4(3 H )‐quinazolinone, drawn attention as promising new class chemotherapeutic agents. addition, showed significant inhibition micromolar ranges when tested vitro against MCF‐7 cell line. this study aims emphasize intriguing versatility halogen atoms, providing an in‐depth summary highlighting developments properties halogenated )‐quinazolinones. It also features detailed discussion structure–activity relationship (SAR) various functional groups their interaction amino acid residues utilizing molecular docking studies. The intent foster novel discoveries can inspire innovative investigations domain. Hence, simplifies design development strategies by prolonging array pharmacologically active candidates.

Language: Английский

Citations

1
Synthesis of Novel Gefitinib-Conjugated 1,2,3-Triazole Derivatives and Their Effect of Inducing DNA Damage and Apoptosis in Tumor Cells DOI Creative Commons

Junfei Wu,

Xu Huang, Shan Lu

et al.

Molecules, Journal Year: 2024, Volume and Issue: 29(22), P. 5438 - 5438

Published: Nov. 18, 2024

Compounds with rigid planar structures can insert into tumor cell DNA, thereby inducing DNA damage in cells. In this study, quinazoline, a compound structure, was used as the core scaffold. A 1,2,3-triazole moiety introduced its and activity tested on HepG2 liver cancer The results showed that most compounds exhibited inhibitory effects cells, IC50 values of effective were 3.08 ± 0.37 μM 3.60 0.53 μM. We found designed significantly upregulated expression γ-H2AX while reducing PARP levels, weakening repair capacity cells leading to apoptosis. Additionally, these inhibited migration invasion One be low toxicity mice, suggesting potential targeted anti-tumor drug.

Language: Английский

Citations

1
Discovery of novel octahydroquinazoline scaffolds endowed with dual inhibition of tubulin polymerization/Eg5 against HCC: Apoptotic and radio-chemotherapeutic studies DOI
Mohammed K. Abdelhameid,

Ehab S. Taher,

Mohammed A. Hara

et al.

Bioorganic Chemistry, Journal Year: 2024, Volume and Issue: 148, P. 107449 - 107449

Published: May 10, 2024

Language: Английский

Citations

0