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Updated: Oct 10, 2025

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
Synthetic and Naturally Occurring Heterocyclic Anticancer Compounds with Multiple Biological Targets
Richard Kwamla Amewu1, Patrick Opare Sakyi1,2, Dorcas Osei-Safo1
1Department of Chemistry, School of Physical and Mathematical Sciences, College of Basic and Applied Sciences, University of Ghana, Legon, Accra P.O. Box LG 56, Ghana.
Abstract:
Cancer is a complex group of diseases initiated by abnormal cell division with the potential of spreading to other parts of the body. The advancement in the discoveries of omics and bio- and cheminformatics has led to the identification of drugs inhibiting putative targets including vascular endothelial growth factor (VEGF) family receptors, fibroblast growth factors (FGF), platelet derived growth factors (PDGF), epidermal growth factor (EGF), thymidine phosphorylase (TP), and neuropeptide Y4 (NY4), amongst others. Drug resistance, systemic toxicity, and drug ineffectiveness for various cancer chemo-treatments are widespread. Due to this, efficient therapeutic agents targeting two or more of the putative targets in different cancer cells are proposed as cutting edge treatments. Heterocyclic compounds, both synthetic and natural products, have, however, contributed immensely to chemotherapeutics for treatments of various diseases, but little is known about such compounds and their multimodal anticancer properties. A compendium of heterocyclic synthetic and natural product multitarget anticancer compounds, their IC50, and biological targets of inhibition are therefore presented in this review.
Insights
This review compiles heterocyclic compounds, both synthetic and natural, that target multiple cancer pathways. It highlights their potential to overcome drug resistance and toxicity in cancer chemotherapy.
Area of Science:
- Oncology
- Medicinal Chemistry
- Bioinformatics
Background:
- Cancer involves abnormal cell division and metastasis.
- Current cancer therapies face challenges like drug resistance, toxicity, and ineffectiveness.
- Targeting multiple cancer pathways offers a promising therapeutic strategy.
Purpose of the Study:
- To present a comprehensive review of heterocyclic compounds with multitarget anticancer properties.
- To compile data on synthetic and natural product-derived heterocyclic compounds.
- To document their inhibitory effects (IC50) and biological targets.
Main Methods:
- Literature review of omics, bioinformatics, and cheminformatics discoveries.
- Identification of drugs targeting key pathways like VEGF, FGF, PDGF, EGF, TP, and NY4.
- Compilation of data on heterocyclic compounds, their IC50 values, and inhibition targets.
Main Results:
- Heterocyclic compounds, from both synthetic and natural sources, show significant anticancer potential.
- These compounds exhibit multimodal activity by inhibiting multiple targets.
- Data on IC50 values and specific biological targets are provided for various compounds.
Conclusions:
- Heterocyclic compounds represent a valuable class of agents for multitarget cancer therapy.
- Their ability to inhibit multiple targets may overcome existing therapeutic limitations.
- This compendium serves as a resource for developing novel anticancer drugs.
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