484692-15-1

Upstream product

• 1121-60-4 pyridine-2-carbaldehyde 
• 504-29-0 2-aminopyridine 
• 931-53-3 Cyclohexyl isocyanide 
• 109-12-6 2-aminopyrimidine 
• 109-06-8 α-picoline 

Relevant academic research and scientific papers

Synthesis of copper and zinc 2-(pyridin-2-yl)imidazo[1,2-a]pyridine complexes and their potential anticancer activity

A small library of novel copper and zinc imidazo[1,2-a]pyridine complexes have been synthesized. Their structures were confirmed by X-ray diffraction crystallography and a selection of these compounds was tested against five cancer cell lines originating from breast cancer (MCF-7 and MDA-MB-231), leukemia (K562 and HL-60) and colorectal cancer (HT-29). The imidazo[1,2-a]pyridines and their zinc complexes showed poor anticancer activity, while the copper complexes were active against the cancer cell lines with IC50values comparable to and lower than camptothecin. For example, copper 6-bromo-N-cyclohexyl-2-(pyridin-2-yl)imidazo[1,2-a]pyridin-3-amine acetate 21 had an IC50value lower than 1 μM against the HT-29 cells. Fluorescence microscopy with acridine orange, Hoechst 33342 and ethidium bromide, used in a preliminary investigation to evaluate morphological changes showed that copper 6-bromo-N-cyclohexyl-2-(pyridin-2-yl)imidazo[1,2-a]pyridin-3-amine acetate 21 caused both apoptosis, necrosis and paraptosis in the MCF-7 and HL-60 cells. A select group of copper N-cyclohexyl-2-(pyridin-2-yl)imidazo[1,2-a]pyridin-3-amines (26, 27, 29 and 31) induced apoptosis, paraptosis and deformed nuclei in MCF-7 cells.

Multiple Multicomponent Reactions: Unexplored Substrates, Selective Processes, and Versatile Chemotypes in Biomedicine

Multiple multicomponent reactions rapidly assemble complex structures. Despite being very productive, the lack of selectivity and the reduced number of viable transformations restrict their general application in synthesis. Hereby, we describe a rationale for a selective version of these processes based in the preferential generation of intermediates which are less reactive than the initial substrates. In this way, applying the Groebke–Blackburn–Bienaymé reaction on a range of α-polyamino-polyazines, we prepared a family compact heterocyclic scaffolds with relevant applications in medicinal and biological chemistry (live cell imaging probes, selective binders for DNA quadruplexes, and antiviral agents against human adenoviruses). The approach has general character and yields complex molecular targets in a selective, tunable and direct manner.

Green synthesis, characterization and antidiabetic activity of 2-substituted aryl/Alkyl-N-Aryl/Alkyl imidazo[1,2-a]pyridin-3-amine derivatives

Imidazo[1,2-a]pyridines containing ring junction have shown broad therapeutic properties in the drug discovery sector, such as the treatment of heart disease, migraines, digestive disease and viral disease. Imidazo[1,2-a]pyridine structure is very much pr

A facile I2-catalyzed synthesis of imidazo[1,2-: A] pyridines via sp3 C-H functionalization of azaarenes and evaluation of anticancer activity

A facile and efficient metal-free, one-pot, three component synthetic protocol has been developed for the synthesis of medicinally important substituted imidazo[1,2-a]pyridines via the iodine-catalysed oxidative amination of benzylic C-H bonds of azaarenes with 2-aminoazines and condensation with isocyanides. The presented methodology offers the advantages of wide substrate scope, moderate reaction conditions, environment friendliness, clean and simple protocol with high atom economy apart from higher yields. The synthesized compounds were screened for their anti-cancer activity in selected human cancer cell lines. Compounds 4a, 4b, 4c, 4i, 7a, 7b and 7m have significant IC50 values ranging from 4.88 ± 0.28 to 14.55 ± 0.74 μM.

IMIDAZO[1,2-A]PYRIDINE COMPLEXES WITH ANTICANCER ACTIVITY

This invention relates to a metal complex of an imidazo[l,2-a]pyridine ligand and/or a metal complex of an imidazo[l,2-a] pyridine ligand derivative and/or an analogue thereof, wherein said metal complexes are for use in treating cancer. Typically, the cancer is breast cancer, colorectal cancer, colon cancer, and/or leukemia.

A highly flexible and efficient ugi-type multicomponent synthesis of versatile n-fused aminoimidazoles

A microwave-promoted highly flexible and efficient Ugi-type multicomponent reaction of heterocyclic amidines with aldehydes and isocyanides catalyzed by zirconium(IV) chloride was developed. The general protocol offered the very reliable synthesis of a li

NON-NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS

Disclosed herein are antiviral agents, in particular non-nucleoside reverse transcriptase inhibitors (NNRTIs) of the formula. Also disclosed are methods of making the NNRTIs, as well as compositions that include such NNRTIs and methods of their use for tr