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Published on: September 22, 2019
Antineoplastic indole-containing compounds with potential VEGFR inhibitory properties
Dalia R Aboshouk1, M Adel Youssef2, Mohamed S Bekheit1
1Department of Pesticide Chemistry, National Research Centre Dokki Giza 12622 Egypt girgisas10@yahoo.com as.girgis@nrc.sci.eg.
Abstract:
Cancer is one of the most significant health challenges worldwide. Various techniques, tools and therapeutics/materials have been developed in the last few decades for the treatment of cancer, together with great interest, funding and efforts from the scientific society. However, all the reported studies and efforts seem insufficient to combat the various types of cancer, especially the advanced ones. The overexpression of tyrosine kinases is associated with cancer proliferation and/or metastasis. VEGF, an important category of tyrosine kinases, and its receptors (VEGFR) are hyper-activated in different cancers. Accordingly, they are known as important factors in the angiogenesis of different tumors and are considered in the development of effective therapeutic approaches for controlling many types of cancer. In this case, targeted therapeutic approaches are preferable to the traditional non-selective approaches to minimize the side effects and drawbacks associated with treatment. Several indole-containing compounds have been identified as effective agents against VEGFR. Herein, we present a summary of the recent indolyl analogs reported within the last decade (2012-2023) with potential antineoplastic and VEGFR inhibitory properties. The most important drugs, natural products, synthesized potent compounds and promising hits/leads are highlighted. Indoles functionalized and conjugated with various heterocycles beside spiroindoles are also considered.
Insights
Targeted cancer therapies show promise, focusing on inhibiting vascular endothelial growth factor receptors (VEGFR). Recent indole-based compounds demonstrate significant potential as anti-cancer agents by targeting VEGFR.
Area of Science:
- Oncology
- Medicinal Chemistry
- Molecular Biology
Background:
- Cancer remains a major global health challenge, with advanced stages often proving resistant to current treatments.
- Overexpression of tyrosine kinases, particularly vascular endothelial growth factor receptors (VEGFR), drives cancer proliferation and angiogenesis.
- Targeted therapies offer advantages over traditional treatments by minimizing side effects and improving efficacy.
Purpose of the Study:
- To review recent (2012-2023) indole-containing compounds with potential anti-cancer and VEGFR inhibitory properties.
- To highlight promising drug candidates, natural products, and synthesized compounds targeting VEGFR.
- To explore functionalized and spirocyclic indole analogs for cancer therapy.
Main Methods:
- Literature review of scientific publications from 2012 to 2023.
- Identification and summarization of studies reporting indole analogs with anti-neoplastic activity.
- Focus on compounds demonstrating inhibition of vascular endothelial growth factor receptors (VEGFR).
Main Results:
- Several indole analogs exhibit significant anti-cancer potential.
- Compounds targeting VEGFR have shown promise in preclinical studies.
- Functionalized indoles, heterocycle conjugates, and spiroindoles are key areas of investigation.
Conclusions:
- Indole derivatives represent a promising class of compounds for developing targeted anti-cancer therapeutics.
- Inhibition of VEGFR by indole analogs is a viable strategy for combating angiogenesis-dependent cancers.
- Continued research into novel indole structures may yield effective treatments for advanced cancers.
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