# Synthesis and biological activities of 3-aminoimidazo[1,2-α]pyridine compounds

**Authors:** Isra Al-Qadi, Michel Hanania, Ismail Warad, Nisreen Al-Hajj, Rand Hazzam, Yousef Salama, Saki Raheem, Nawaf Al-Maharik

PMC · DOI: 10.1186/s13065-025-01412-6 · 2025-02-22

## TL;DR

This paper reports the synthesis of new 3-aminoimidazo[1,2-α]pyridine compounds and their potential as anticancer agents based on cytotoxicity tests.

## Contribution

The novel contribution is the synthesis and evaluation of eleven new 3-aminoimidazo[1,2-α]pyridine compounds for anticancer activity.

## Key findings

- Compound 12 showed the highest inhibitory activity against HT-29 cancer cells with an IC50 of 4.15 ± 2.93 µM.
- Compound 14 demonstrated promising activity against B16F10 cancer cells with an IC50 of 21.75 ± 0.81 µM.
- Only compounds 12 and 14 exhibited significant inhibitory activity among the eleven synthesized compounds.

## Abstract

Despite their importance in cancer treatment, anticancer compounds face significant challenges due to drug resistance and low specificity, creating an urgent need for the discovery of more effective alternative. Herein, we report the synthesis of eleven 3-aminoimidazole[1,2-α]pyridine compounds (9–19) employing the one-pot Groebke-Blackburn-Bienayme three-component reaction (GBB-3CR). The cytotoxicity of the synthesised compounds was evaluated against three cancer cell lines (MCF-7, HT-29, B16F10) and a normal cell (MEF). Considering effectiveness and safety, the results demonstrated that among the eleven synthesised compounds, only compounds 12 and 14 exhibited high inhibitory activity against cancer cell lines. Compound 12 with a nitro group at the C-2 position and a p-chlorophenyl group at C-3 position, showed the highest inhibitory activity against HT-29, with an IC50 of 4.15 ± 2.93 µM. Additionally, compound 14, with a tolyl moiety at the C-2 position and a p-chlorophenyl amine at C-3 position, can also be considered a promising bioactive product against B16F10, with an IC50 of 21.75 ± 0.81 µM. Further research on these compounds may yield more potent candidates for the development of new anticancer agents.

The online version contains supplementary material available at 10.1186/s13065-025-01412-6.

## Linked entities

- **Chemicals:** 3-aminoimidazo[1,2-α]pyridine (PubChem CID 432221), compound 12 (PubChem CID 122516950), compound 14 (PubChem CID 17753356), p-chlorophenyl (PubChem CID 7697)
- **Diseases:** cancer (MONDO:0004992)

## Full-text entities

- **Diseases:** cytotoxicity (MESH:D064420), cancer (MESH:D009369)
- **Chemicals:** 3-aminoimidazo[1,2-alpha]pyridine (-), p-chlorophenyl amine (MESH:C004658)
- **Cell lines:** B16F10 — Mus musculus (Mouse), Mouse melanoma, Cancer cell line (CVCL_0159), MCF-7 — Homo sapiens (Human), Invasive breast carcinoma of no special type, Cancer cell line (CVCL_0031), MEF — Mus musculus (Mouse), Finite cell line (CVCL_9115), HT-29 — Homo sapiens (Human), Colon adenocarcinoma, Cancer cell line (CVCL_0320)

## Figures

9 figures with captions in the complete paper: https://tomesphere.com/paper/PMC11847391/full.md

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Source: https://tomesphere.com/paper/PMC11847391