Evaluation of the bioactivity of novel spiroisoxazoline typecompounds against normal and cancer cell lines

The aim of this study was to investigate the in vitro cellular activity of novel spiroisoxazoline type compounds against normal and cancer cell lines from lung tissue (Hs888Lu), neuron-phenotypic cells (SH-SY5Y), neuroblastoma (SH-SY5Y), human histiocytic lymphoma (U937), lung cancer (A549), and leukaemia (HL-60). Our bioassay program revealed that the spiroisoxazoline type compounds show cytotoxicity only in lymphoma cell lines, which is in contrast with the pyrrolidine precursor of these spiroisoxazoline compounds, where significant cytotoxicity is seen in all normal and cancer cell lines. These data suggest a tumour-specific mechanism of action. In addition these data also show that spiroisoxazoline compounds are non-toxic in the human neuronphenotypic neuroblastoma SH-SY5Y cell line, and furthermore that they might protect cells from neurodegenerative disease.     

A Short and Elegant Synthesis of (±)‐Streptopyrrolidine

A brief and efficient approach for the synthesis of (±)‐5‐benzyl‐4‐hydroxy‐2‐pyrrolidine ( 1 ) from phenylalanine racemate is described. The key step is the stereocontrolled reduction of the keto functionality of benzylated pyrrolidinone intermediate ( 6 ) via sodium borohydride in carboxylic acid medium furnishing both (R,R)‐ and (S,S)‐configured diastereomers. The natural (R,R) enantiomer ( 2 ), however, crystallized out from its racemic mixture. Structure of 2 was confirmed by NMR, IR, elemental analyzer, and single crystal X‐ray crystallographic techniques.     

Synthesis of 3,4‐Fused γ‐Lactone‐γ‐Lactam Bicyclic Moieties as Multifunctional Synthons for Bioactive Molecules

A short approach for the synthesis of 3,4‐fused γ‐lactone‐γ‐lactam bicyclic systems ( 1 ) in diastereomeric mixtures from chiral D ‐alanine methyl ester hydrochloride is described. The key step towards lactonisation is the reduction of the carbonyl ketone of the 5R‐configured 3,5‐dimethylpyrrolidine‐2,4‐dione diastereomers ( 8 ) via sodium borohydride in the presence of hydrochloric acid. With the presence of ethyl acetyl functionality at C3‐position, ester hydrolysis of 8 occurred concomitantly with keto reduction leading to lactonisation and eventually affording the anticipated (3S,4S,5R), (3R,4R,5R), (3R,4S,5R) and (3S,4R,5R) bicyclic moieties. The formation of the fused systems was confirmed by mass spectroscopy (MS) and nuclear magnetic resonance (NMR) analyses.     

Facile Reduction of β-Enamino Oxopyrrolidine Carboxylates Mediated by Heterogeneous Palladium Catalyst

Russian Journal of Organic Chemistry - The synthesis of diastereoisomers via diastereoselective hydrogenation of unreactive endocyclic enamine system of ethyl 4-hydrazinyl- and...     

MEH-PPV/Alq_3-based bulk heterojunction photodetector

In this paper, we present the effect of varied illumination levels on the electrical properties of the organic blend bulk heterojuction （BHJ） photodiode. To prepare the BHJ blend, poly（2-methoxy-5（2P-ethylhexyloxy） phenyleneviny- lene （MEH-PPV） and aluminum-tris-（8-hydroxyquinoline） （Alq3） are used as donor and acceptor materials, respectively. In order to fabricate the photodiode, a 40-nm thick film of poly（3, 4-ethylendioxytbiophene）：poly（styrensulfonate） （PE- DOT：PSS） is primarily deposited on a cleaned ITO coated glass substrate by spin coating technique. The organic photo- sensitive blend is later spun coated on the PEDOT：PSS layer, followed by the lithium fluoride （LiF） and aluminium （A1） thin films deposition by thermal evaporation. The optical properties of the MEH-PPV：Alq3 blend thin films are investigated using photoluminescence （PL） and UV-Vis spectroscopy. The photodiode shows good photo-current response as a function of variable illumination levels. The responsivity value - 8 mA/W at 3 V is found and the ratio of photo-current to dark current （lph/IDark） is found to be 1.24.