Antineoplastic indole-containing compounds with potential VEGFR inhibitory properties

Aboshouk, Dalia R.; Youssef, M. Adel; Bekheit, Mohamed S.; Hamed, Ahmed R.; Girgis, Adel S.

doi:10.1039/d3ra08962b

RSC Adv.

2024

DOI: 10.1039/d3ra08962b

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Antineoplastic indole-containing compounds with potential VEGFR inhibitory properties

Dalia R. Aboshouk,

M. Adel Youssef,

Mohamed S. Bekheit

et al.

Abstract: VEGF, an important category of tyrosine kinases, and its receptors (VEGFR) are hyper-activated in different cancers. The recently reported indolyl analogs with potential antineoplastic and VEGFR inhibitory properties are highlighted.

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Cited by 7 publications

References 145 publications

(213 reference statements)

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Design, Synthesis, Anti‐Cancer, Anti‐Inflammatory and In Silico Studies of 3‐Substituted‐2‐Oxindole Derivatives

Hublikar,

Kadu,

Edake

et al. 2024

Chemistry & Biodiversity

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This study focuses on the design and multistep synthesis of diverse structural and functional 3‐substituted‐2‐oxindole derivatives aimed at being dual‐active molecules with anti‐cancer and anti‐inflammatory properties. In vitro evaluations confirmed the dual activity of these derivatives. 4a exhibited GI50 value 3.00E‐05 against MDA‐MB‐231; 4b has shown GI50 value 2E‐05 against MDA‐MB‐231; 4c has shown GI50 value 6E‐05 against VERO; and 4d has shown GI50 value 8E‐05 each against both MDA‐MB‐231 and MCF‐7. 4e has shown GI50 values 2E‐05 and 5E‐05 each against both the MCF‐7 and VERO. The analysis indicates that compounds 3c (71.19%), 3e (66.84%), and 3g (63.04%) exhibited significant anti‐inflammatory activity. Additionally, in silico binding free energy analysis and interaction studies revealed significant correlations between in vitro and computational data, identifying compounds 4d, 4e, 3b, 3i, and 3e as promising candidates. Key residues such as Glu917, Cys919, Lys920, Glu850, Lys838, and Asp1046 were found to play critical roles in ligand binding and kinase inhibition, providing valuable insights for designing potent VEGFR2 inhibitors. The quantum mechanics‐based independent gradient model analysis further highlighted the electronic interaction landscape, showing larger attractive peaks and higher electron density gradients for compounds 4d and 4e compared to Sunitinib, suggesting stronger and diverse attractive forces.

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Design, Synthesis, Anti‐Cancer, Anti‐Inflammatory and In Silico Studies of 3‐Substituted‐2‐Oxindole Derivatives

Hublikar,

Kadu,

Edake

et al. 2024

Chemistry & Biodiversity

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show abstract

Development of 3-indolyl substituted phenyl pyrazolo-carboxamide hybrids as potential type II VEGFR-2 inhibitors and in vitro cytotoxicity studies

Valapil,

Devabattula,

Barahdia

et al. 2025

Bioorganic & Medicinal Chemistry Letters

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Synthesis and anti-tumor activity of new benzofuran-based chalcone derivatives as potent VEGFR-2 inhibitors

Zhang,

Liu,

Zhang

et al. 2025

RSC Med. Chem.

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Antineoplastic indole-containing compounds with potential VEGFR inhibitory properties

Abstract: VEGF, an important category of tyrosine kinases, and its receptors (VEGFR) are hyper-activated in different cancers. The recently reported indolyl analogs with potential antineoplastic and VEGFR inhibitory properties are highlighted.

Cited by 7 publications

References 145 publications

Design, Synthesis, Anti‐Cancer, Anti‐Inflammatory and In Silico Studies of 3‐Substituted‐2‐Oxindole Derivatives

Design, Synthesis, Anti‐Cancer, Anti‐Inflammatory and In Silico Studies of 3‐Substituted‐2‐Oxindole Derivatives

Development of 3-indolyl substituted phenyl pyrazolo-carboxamide hybrids as potential type II VEGFR-2 inhibitors and in vitro cytotoxicity studies

Synthesis and anti-tumor activity of new benzofuran-based chalcone derivatives as potent VEGFR-2 inhibitors

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