Imidazo[1,2-a]pyridines: Promising Drug Candidate for Antitumor Therapy

Abstract

Imidazo[1,2-a]pyridine has been shown to be an important biologically active moiety. This review is a compilation of the scattered output of results of the anticancer activities of the imidazo[1,2-a]pyridine system since 2001, which have been classified as inhibition of CDK, VEGFR, PI3K, EGFR, RGGT etc. along with inhibition against different tumor cell lines. Various imidazo[1,2-a]pyridine based analogues have been used as lead molecules and are now under human clinical trials. This review will help the wider scientific community in the area of drug discovery of imidazo[1,2-a]pyridines as novel anticancer agents.

Novel imidazo[1,2‑a]pyridine inhibits AKT/mTOR pathway and induces cell cycle arrest and apoptosis in melanoma and cervical cancer cells

“…In particular, the imidazo[1,2-a]pyridine moieties of imidazopyridine have recently gained significant interest as potential anticancer agents due to their potent inhibitory role of cancer cell growth, which is commonly due to survival kinases inhibition (7,8). Various drugs containing imidazo[1,2-a]pyridine moieties are currently used to treat cardiac disorders, insomnia, antianxiety, ulcers and HIV infections (9). Although these compounds have numerous medicinal applications, none of them have been accepted as an anti-cancer drug.…”

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“…The compounds were also synthesized in the conventional method (7), and the yield of each compound was compared with the authentic samples. It has been observed that the yield of all the compounds was increased in microwaveassisted synthesis method.…”

Crystal structure, Hirshfeld surface analysis and contact enrichment ratios of 1-(2,7-dimethylimidazo[1,2-a]pyridin-3-yl)-2-(1,3-dithiolan-2-ylidene)ethanone monohydrate

“…Compounds with the imidazo[1,2-a]pyridine scaffold exhibit a plethora of biological activities, including acting as receptor ligands, anti-infectious agents, enzyme inhibitors etc. as well as being potential nitrogen heterobicycle therapeutic agents, as described by recent studies (Goel et al, 2016;Deep et al, 2017;Kuthyala et al, 2018). On the other hand, compounds containing the 1,3-dithiolan-2-ylidene moiety have been found to exhibit valuable pharmacological activities, including use as potent broad-spectrum fungicides (Tanaka et al, 1976, Wang et al, 1994, antitumor agents (Huang et al, 2009), potent cephalosporinase inhibitors (Ohya et al, 1982) and anti-HIV agents (Nguyen-Ba et al, 1999;Besra et al, 2005).…”