Synthesis and anti-cancer activity of 1,4-disubstituted imidazo[4,5-c]quinolines.

The synthesis and anti-cancer activity evaluation of fused imidazoquinoline compounds is reported in this paper. Yb(OTf)3 has been utilized as a catalyst for the synthesis of 1,4-diaryl substituted imidazo[4,5-c]quinolines via a modified Pictet-Spengler approach. The desired imidazole ring was synthesized from imines using TosMIC (toluenesulfonylmethyl isocyanide) and subsequently functionalized at the C-4 position yielding an imidazoquinoline skeleton. Importantly, the final step was carried out without the aid of any prefunctionalization to obtain the resultant compounds in good yields. The synthesized compounds, when screened for anti-cancer activity, revealed the highest activity with 4-(2-bromophenyl)-1-phenyl-1H-imidazo[4,5-c]quinoline (IC50: 103.3 µM).

Synthesis of 4-substituted oxazolo[4,5-c]quinolines by direct reaction at the C-4 position of oxazoles.

A facile synthesis of 4-aryl substituted oxazolo[4,5-c]quinolines has been described via a modified Pictet-Spengler method and using Cu(TFA)2 as a catalyst. The developed methodology directly functionalizes the C-4 position of oxazoles without the aid of any prefunctionalization, in the presence of the more reactive C-2 position in good yields. The versatility of the established method has been demonstrated by its application in the synthesis of 4-substituted oxazolo-[1,8]naphthyridine ring systems.

The Birmingham hip resurfacing prosthesis: an independent single surgeon's experience at 7-year follow-up.

An independent single surgeon's 7-year experience with Birmingham hip resurfacing is presented. The study also involved investigation of the significance of pedestal sign in patients requiring revision. A consecutive 117 hips in 101 patients (59 male and 42 female patients) operated on by the senior author (VGJ) were assessed at a mean follow-up of 7 years (range, 5-9.4 years). Mean age at surgery was 54 years (range, 20-74 years). Seventy-three hips had a preoperative diagnosis of primary osteoarthritis, and secondary osteoarthritis was seen in 44 hips. Failure was defined as revision for any reason. Revision of the femoral component alone was undertaken in 8 hips (6.8%): 5 within first year for periprosthetic fracture neck of femur and in 3 hips after 5 years of follow-up. In 2 patients who were known to have osteonecrosis of the femoral head preoperatively, the femoral component progressively collapsed into varus after 5 years of follow-up. Pedestal sign was the earliest radiologic sign noted in these 2 patients and progressed rapidly within 1 year on serial radiographs well before the onset of clinical symptoms. Kaplan-Meier survival with revision as end point at 7 years was 91.5% (95% confidence interval, 97.6%-85.4%).

Immobilized lipase from Lactobacillus plantarum in meat degradation and synthesis of flavor esters.

Microbial lipases owing to their broad substrate specificity are widely used in various industrial applications like food processing, organic synthesis, detergent formulation and oil manufacturing. In the current study the immobilized lipase from Lactobacillus plantarum was found novel in degrading meat which can be applied in medical field and also in synthesizing different short chain fatty acid esters like 2,3,4-hydroxybenzyl acetates and triazole ester which makes a great impingement in natural flavor industry. The 4-hydroxybenzyl acetate obtained can also be used in cosmetics.

Zinc(II) Ion Sensing in Aqueous Micellar Solution Using Modified Bipyridine-Based "Turn-On" Fluorescent Probes and its Application in Bioimaging.

The bipyridine-based constructs 4-(pyridine-2-yl)-3H-pyrrolo[2,3-c]quinoline (PPQ) and [6-(3H-pyrrolo[2,3-c]quinolin-4-yl)pyridin-2-yl]methanol (PPQ-OH) and their assemblies with surfactants are evaluated as turn-on fluorescent sensors for Zn2+ ions in aqueous solution. This study strives to overcome the problem of low water solubility of the hydrophobic PPQ and PPQ-OH by using micelles. Whereas the ligands show selective sensing behavior for Zn2+ over important biological cations including Na+ , K+ , Ca2+ , Mg2+ in anionic sodium dodecyl sulfate and non-ionic Tween 80 micelles, no Zn2+ sensing is observed in cationic cetyltrimethylammonium bromide micelles. Unlike in DMF, Cd2+ interference is observed in aqueous conditions, which can be avoided either by performing the study at pH≥9 or by carrying out a time-resolved fluorescence study. Analysis of the Job plot data, the fluorescence lifetimes, and experiments on varying micellar shape and pH, confirms that the coordination volume of the resulting octahedral metal complex and formation of a five-membered chelate ring are critical factors for Cd2+ interference. The described sensing systems are capable of detecting Zn2+ ions at the micromolar level. Additionally, it is shown that PPQ and PPQ-OH can be used to detect Zn2+ in HeLa cells under physiological conditions in bioimaging studies.