# Coumarin–Dithiocarbamate Derivatives as Biological Agents

**Authors:** Piotr Wiliński, Aleksander Kurzątkowski, Kinga Ostrowska

PMC · DOI: 10.3390/ijms26199667 · 2025-10-03

## TL;DR

This paper reviews recent advances in coumarin-dithiocarbamate compounds, highlighting their diverse biological activities including anticancer and antimicrobial effects.

## Contribution

The paper provides a focused review exclusively on coumarin-dithiocarbamate derivatives and their biological activities.

## Key findings

- Coumarin-dithiocarbamate derivatives show cytotoxic activity against multiple human cancer cell lines.
- These derivatives inhibit acetylcholinesterase and monoamine oxidases, suggesting potential CNS activity.
- They also exhibit α-glucosidase inhibition and antimicrobial properties.

## Abstract

Coumarin derivatives, whether natural or synthetic, have attracted considerable interest from medicinal chemists due to their versatile biological properties. Their appealing pharmacological activities—such as anticancer, anti-inflammatory, neuroprotective, anticoagulant, and antioxidant effects—combined with the ease of their synthesis and the ability to introduce chemical modifications at multiple positions have made them a widely explored class of compounds. In the scientific literature, there are many examples. On the other hand, dithiocarbamates, originally employed as pesticides and fungicides in agriculture, have recently emerged as potential therapeutic agents for the treatment of serious diseases such as cancer and microbial infections. Moreover, dithiocarbamates bearing diverse organic functionalities have demonstrated significant antifungal properties against resistant phytopathogenic fungi, presenting a promising approach to combat the growing global issue of fungal resistance. Dithiocarbamates linked to coumarin derivatives have been shown to exhibit cytotoxic activity against various human cancer cell lines, including MGC-803 (gastric), MCF-7 (breast), PC-3 (prostate), EC-109 (esophageal), H460 (non-small cell lung), HCCLM-7 (hepatocellular carcinoma), HeLa (cervical carcinoma), MDA-MB-435S (mammary adenocarcinoma), SW480 (colon carcinoma), and Hep-2 (laryngeal carcinoma). Numerous studies have revealed that the inclusion of a dithiocarbamate moiety can provide central nervous system (CNS) activity, particularly through inhibitory potency and selectivity toward acetylcholinesterase (AChE) and monoamine oxidases (MAO-A and MAO-B). Recently, it has been reported that coumarin–dithiocarbamate derivatives exhibit α-glucosidase inhibitory effects and also possess promising antimicrobial activity. This study presents an overview of recent progress in the chemistry of coumarin–dithiocarbamate derivatives, with a focus on their biological activity. Previous review papers focused on coumarin derivatives as multitarget compounds for neurodegenerative diseases and described various types of compounds, with dithiocarbamate derivatives representing only a small part of them. Our work deals exclusively with coumarin dithiocarbamates and their biological activity.

## Linked entities

- **Proteins:** MAOA (monoamine oxidase A), MAOB (monoamine oxidase B)
- **Chemicals:** coumarin (PubChem CID 323), dithiocarbamate (PubChem CID 3001860)
- **Diseases:** cancer (MONDO:0004992)

## Full-text entities

- **Genes:** ACHE (acetylcholinesterase (Yt blood group)) [NCBI Gene 43] {aka ACEE, ARACHE, N-ACHE, YT}, SI (sucrase-isomaltase) [NCBI Gene 6476], MAOA (monoamine oxidase A) [NCBI Gene 4128] {aka BRNRS, MAO-A}, MAOB (monoamine oxidase B) [NCBI Gene 4129]
- **Diseases:** cancer (MESH:D009369), neurodegenerative diseases (MESH:D019636), colon carcinoma (MESH:D003110), gastric (MESH:D013272), inflammatory (MESH:D007249), fungal (MESH:D009181), esophageal (MESH:D004941), breast (MESH:D061325), hepatocellular carcinoma (MESH:D006528), cervical carcinoma (MESH:D002583), non-small cell lung (MESH:D002289), mammary adenocarcinoma (MESH:D000230), microbial infections (MESH:D015163), laryngeal carcinoma (MESH:D007822), prostate (MESH:D011472)
- **Chemicals:** Coumarin-Dithiocarbamate (-), Coumarin (MESH:C030123)
- **Species:** Homo sapiens (human, species) [taxon 9606]
- **Cell lines:** MGC-803 — Homo sapiens (Human), Hybrid cell line (CVCL_5334), SW480 — Homo sapiens (Human), Colon adenocarcinoma, Cancer cell line (CVCL_0546), HeLa — Homo sapiens (Human), Human papillomavirus-related endocervical adenocarcinoma, Cancer cell line (CVCL_0030), MCF-7 — Homo sapiens (Human), Invasive breast carcinoma of no special type, Cancer cell line (CVCL_0031), MDA-MB-435S — Homo sapiens (Human), Amelanotic melanoma, Cancer cell line (CVCL_0622), EC-109 — Homo sapiens (Human), Esophageal squamous cell carcinoma, Cancer cell line (CVCL_6898), HCCLM-7 — Homo sapiens (Human), Adult hepatocellular carcinoma, Cancer cell line (CVCL_6832), H460 — Homo sapiens (Human), Lung large cell carcinoma, Cancer cell line (CVCL_0459), Hep-2 — Homo sapiens (Human), Human papillomavirus-related endocervical adenocarcinoma, Cancer cell line (CVCL_1906), PC-3 — Homo sapiens (Human), Prostate carcinoma, Cancer cell line (CVCL_0035)

## Figures

17 figures with captions in the complete paper: https://tomesphere.com/paper/PMC12524870/full.md

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Source: https://tomesphere.com/paper/PMC12524870