The Anticancer Effects of Novel Imidazo[1,2-a]Pyridine Compounds against HCC1937 Breast Cancer Cells.

Background: Anticancer drugs confront clinical obstacles such as drug resistance and adverse effects. Imidazo[1,2-a]pyridines (IPs) compounds have lately gained considerable interest as possible anticancer therapeutics due to their potent inhibitory function against cancers cells. This study was to determine the anticancer activities of three novel IPs (IP-5, IP-6, and IP-7) against the HCC1937 breast cancer cell line in vitro.

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

The present study aimed to investigate the anti-cancer activity of imidazo[1,2-a]pyridine 5-7 in the A375 and WM115 melanoma and HeLa cervical cancer cell lines. The viability of cancer cells was analyzed by the MTT assay. Apoptosis was quantified by flow cytometry following staining of the cells with AnnexinV/propidium iodide (PI).

Inversion dimers dominate the crystal packing in the structure of trimethyl citrate (trimethyl 2-hy-droxy-propane-1,2,3-tri-carboxyl-ate).

Trimethyl citrate, CHO (systematic name: trimethyl 2-hy-droxy-propane-1,2,3-tri-carboxyl-ate), , was prepared by the esterification of citric acid and methanol in the presence of thionyl chloride at 273 K. The bond lengths and angles in compare closely with those observed in citric acid. The C-C bonds adjacent to the terminal carboxyl groups are significantly shorter than those around the central C atom.

Synthesis, antibacterial and QSAR evaluation of 5-oxo and 5-thio derivatives of 1,4-disubstituted tetrazoles.

A series of 1,4-disubstituted tetrazol-5-ones 3a, 5, 7, 12, 13 and 1,4-disubstituted tetrazol-5-thiones 3b, 9, 10 was synthesized and fully characterized by IR, MS, (1)H NMR and (13)C NMR. The series was evaluated for in vitro antibacterial activity against four Gram negative (Escherichia coli, Proteus mirabilis, Klebsiella pneumonia, and Pseudomonas aeruginosa) and three Gram positive (Staphylococcus aureus, Enterococcus faecalis, and Bacillus subtilis) bacteria. The zone of inhibition was measured using the well-diffusion assay, and in vitro minimum inhibitory concentration (MIC) was determined by microbroth dilution assay.

Antibacterial activities of novel nicotinic acid hydrazides and their conversion into N-acetyl-1,3,4-oxadiazoles.

Synthesis of a series of novel N-acylhydrazones of nicotinic acid hydrazides 3a-j via condensation of nicotinic acid hydrazide 1 with the corresponding aldehydes and ketones is described. The series 3a-j was evaluated for in vitro antibacterial activity against two gram negative (Pseudomonas aeruginosa and Klebsiella pneumoniae) and two gram positive (Streptococcus pneumoniae and Staphylococcus aureus) bacteria. The zone of inhibition was measured using the disk diffusion method, and in vitro minimum inhibitory concentration indicating that compounds 3a and 3e were effective against P.

(Z)-1-Chloro-1-[2-(2-nitro-phen-yl)hydrazinyl-idene]propan-2-one.

The title mol-ecule, C9H8ClN3O3, lies on a mirror plane. Intra-molecular N-H⋯O and N-H⋯Cl hydrogen bonds occur. One of the nitro O atoms is disordered (site occupancy ratio = 0.

Reaction of nitrilimines with 2-substituted aza-heterocycles. Synthesis of pyrrolo[1,2-a]pyridine and pyrimido[2,1-d]1,2,3,5- tetrazine.

The reaction of nitrilimine 6a with ethyl pyridine-2-acetate (7) gave the corresponding pyrrolo[1,2-a]pyridine 8, while the reaction of 6b containing an ester moiety afforded the acyclic adduct 9. The reaction of 6a with 2-aminopyrimidine (10) gave the novel unexpected pyrimido[2,1-d]1,2,3,5-tetrazine 11. Acyclic adducts 16 and 17 were obtained from the reaction of 6b with 2-cyanomethylbenzimidazole (14) and 2-aminobenzimidazole (15), respectively.

Reaction of nitrilimines and nitrile oxides with hydrazines, hydrazones and oximes.

This review article discusses the reaction of nitrilimines and nitrile oxides with hydrazines, hydrazones, and oximes. Three reaction modes were observed. The article mainly covers our work published over the last fifteen years, in which interesting heterocyles such as oxadiazoles, triazoles, and tetrazines were synthesized and fully characterized.