InCl 3 -Catalyzed [2+3] Cycloaddition Reaction: A Rapid Synthesis of 5-Substituted 1H-tetrazole under Microwave Irradiation

Abstract: A series of 5-substituted 1H-tetrazole were efficiently prepared by InCl 3 catalyzed (10 mol %) from structurally divert organic nitriles with sodium azide under the influence of microwave irradiation. The present protocol was successfully applied to the aliphatic, aryl, benzylic and heterocyclic nitriles and corresponding 5-substituted 1H-tetrazole were obtained in good to excellent yield (70-96%). This method gives remarkable advantages such as short reaction time, simple work-up procedure and economical beneficial

Phosphonic acid appended naphthalenediimide molecular receptor for saccharides and aminoglycoside antibiotics recognition

Design of symmetric phosphonic acid functionalized naphthalene diimide bolaamphiphile (NDI 1) is reported. NDI 1 based molecular recognition of saccharides and aminoglycoside antibiotics in aqueous media was investigated. UV-vis and fluorescence measurements revealed an efficient protocol for NDI 1 as molecular receptor. The sensor successfully recognises saccharides and aminoglycoside antibiotics kanamycin and neomycin in terms of both absorbance intensity and binding affinity. This protocol provides new platform for the design and synthesis of phosphonic acid appended NDI sensor for recognition of multifunctional biomolecules

Design and synthesis of phosphonate functionalized naphthalenediimide: Application to induce mitochondria mediated apoptosis in the human skin melanoma cells (SKMEL2)

506-512New phosphonate functionalized naphthalenediimides (NDI-1 and NDI-2) have been synthesized and evaluated as potential drug candidates to treat the skin malignancy. The aforementioned candidates have resulted in an induced apoptosis pathway of cytotoxicity, at concentrations lower than 4 μM, in human skin melanoma cells, and elicited a stronger apoptotic response in cells. Regulation of the Bcl2, Caspases, Bak1, Bax protein in NDI-induced apoptosis in cells has been analyzed by real time PCR, and the cell viability and apoptosis determined by flow cytometry. The obtained results indicate that NDIinduced apoptosis by regulation of Bcl2 and Bak1 occurs in human skin melanoma cells (SKMEL-2)

Organogelation and cytotoxic evolution of phosphonate ester functionalised hydrophobic alkanediamide motifs

<div><p>Here we report various rigid alkanediamide derivatives, with three different substitution patterns of phosphonate ester for investigation of organogelation properties. The gelation properties of these compounds can be tuned by altering the number and position of the phosphonate esters. It was found that supramolecular self-assembly of the bisphosphonate esters (<b>1a, 1d, 1h</b> and <b>2a</b>–<b>b</b>) resulted gel formation, whereas that of the tetraphosphonate esters (<b>3a, 3d, 3h</b>) resulted in construction of nanospheres and microspheres. The diverse morphology of the gel formation appears to depend predominantly on the substituted phenyl ring of the phosphonate ester functionality. Subsequent <i>in vitro</i> cytotoxic screening against four human tumour cell lines (A549, MDA-MB-231, MCF-7 and HeLa) using MTT assays revealed that derivatives <b>1f</b>–<b>h</b> and <b>3a</b> show cytotoxic potencies at concentrations less than 5 μM (IC₅₀ values). Compounds <b>1f</b>–<b>h</b> exhibited promising activity against A549 cell line, <b>1g</b>–<b>h</b> were highly effective against MDA-MB-231, <b>1f</b> and <b>3a</b> show potential against MCF-7 and <b>1f</b>–<b>g</b> were active against the HeLa cell line.</p></div