Synthesis and biological activities of 3-aminoimidazo[1,2-α]pyridine compounds
Isra Al-Qadi, Michel Hanania, Ismail Warad, Nisreen Al-Hajj, Rand Hazzam, Yousef Salama, Saki Raheem, Nawaf Al-Maharik
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.
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…
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Taxonomy
TopicsSynthesis and Reactivity of Heterocycles · Cancer therapeutics and mechanisms · Synthesis and Characterization of Heterocyclic Compounds