Two new isoflavanoids from the rhizomes of Iris soforana

Two new isoflavones 1 and 2 along with eleven known compounds 3-13, have been isolated for the first time from the rhizomes of Iris soforana. The structures of these compounds were determined on the basis of spectroscopic methods and found to be 5,3'-dihydroxy-4'-methoxy-6,7-methylenedioxyisoflavone (1) (Soforanarin A), and 5,7,5'-trimethoxy-6,3',4'-trihydroxyisoflavone (2) (Soforanarin B).     

Purification of hyaluronidase as an anticancer agent inhibiting CD44

Hyaluronidase (Hyal) can be employed to accomplish a diversity of complications related to hyaluronic acid (HA). Hyal contains some classes of catalysts that cleave HA. This enzyme is detected in several human tissues as well as in animal venoms, pathogenic organisms and cancers. Destructive cancer cells regularly increase the CD44 receptor existing in a cell membrane. This receptor acts as an exact receptor for HA, and HA is recognized to motivate the migration, spread, attack and metastasis of cancer cells. Nearly all of the methods used to purify Hyal are highly costly and not proper for industrial applications. This survey aims to review different methods of Hyal purification, which acts as an anticancer agent by degrading HA in tissues and thus inhibiting the CD44–HA interaction. Hyal can be successfully employed in the management of cancer, which is associated with HA–CD44. This review has described different methods for Hyal purification to prepare an origin to develop a novel purification technique for this highly appreciated protein. Using multiple columns is not applicable for the purification of Hyal and thus cannot be used at the industrial level. It is better to use affinity chromatography of anti-Hyal for Hyal with one-step purification.     

An Efficient,One-Pot Synthesis of Dialkyl 5-Hydroxy-4-aryl-2,5-dihydrofuran-2,3-dicarboxylate Derivatives

The reaction between arylglyoxalmonohydrates, dialkyl acetylenedicarboxylates, and triphenylphosphine is described as a simple and efficient method for the synthesis of 5-hydroxy-4-aryl-2,5-dihydrofuran-2,3-dicarboxylate derivatives.     

Identification of Compounds that Selectively Stabilize Specific G‐Quadruplex Structures by Using a Thioflavin T‐Displacement Assay as a Tool

Small molecules are used in the G‐quadruplex (G4) research field in vivo and in vitro, and there are increasing demands for ligands that selectively stabilize different G4 structures. Thioflavin T (ThT) emits an enhanced fluorescence signal when binding to G4 structures. Herein, we show that ThT can be competitively displaced by the binding of small molecules to G4 structures and develop a ThT‐displacement high‐throughput screening assay to find novel and selective G4‐binding compounds. We screened approximately 28 000 compounds by using three different G4 structures and identified eight novel G4 binders. Analysis of the structural conformation and stability of the G4 structures in presence of these compounds demonstrated that the four compounds enhance the thermal stabilization of the structures without affecting their structural conformation. In addition, all four compounds also increased the G4‐structure block of DNA synthesis by Taq DNA polymerase. Also, two of these compounds showed selectivity between certain Schizosaccharomyces pombe G4 structures, thus suggesting that these compounds or their analogues can be used as selective tools for G4 DNA studies.     

Rotaxane‐Like Structures Threaded through the Pores of Hollow Porous Nanocapusles

Nanocapsules with molecules threaded through the porous shells may lead to advanced cell‐mimicking functional devices. Herein, we show the feasibility of synthesizing such hybrid nanostructures by using vesicle‐templated polymer nanocapsules with controlled nanopores. Ship‐in‐a‐bottle assembly inside a nanocapsule created an internal unit. An external unit was then connected to an entrapped internal unit through pre‐attached linker threaded through a nanopore in the shell of the nanocapsule. Both internal and external units are larger than the pore size and cannot cross the shell, producing a rotaxane‐like structure. Successful synthesis was achieved with fairly short linkers (six and ten carbon atoms in a chain), creating an opportunity for facile synthesis of functional devices capable of cross‐shell communication.     

Facile microwave route for the synthesis of CuS/CQDs/g-C3N4NS as a novel promising cathodic electrochemiluminescence detection of imidacloprid

Journal of Solid State Electrochemistry - In this study, a novel electrochemical luminescence based on ternary nanocomposite as CuS/CQDs/g-C3N4NS was demonstrated for accurate determination of...     

One-Pot Synthesis of Novel Rhodanine Based Ketenimines Via Multicomponent Reactions

Abstract

Synthesis of polyfunctionalized ketenimines via three-component reactions of rhodanine and 5-(4-dimethylaminobenzylidene)-rhodanine with dialkyl acetylenedicarboxylates and alkyl isocyanides is described. The reactions proceed smoothly under mild conditions leading to the desired products in good yields. In the case of methyl acetylenecarboxylate, the reaction led to methyl (Z)-3-({5-[(E)-1-(tert-butylamino)methylidene]-4-oxo-4,5-dihydro-1,3-thiazol-2-yl}sulfanyl)-2-propenoate in low yield.

GRAPHICAL ABSTRACT      

Radiosynthesis and biological evaluation of 166Ho labeled methoxylated porphyrins as possible therapeutic agents

¹⁶⁶Ho labeled 5,10,15,20-tetrakis(3,4-dimethoxyphenyl) porphyrin, and 5,10,15,20-tetrakis(3,4,5-trimethoxyphenyl) porphyrin ([¹⁶⁶Ho]–TDMPP and [¹⁶⁶Ho]–TTMPP respectively) were prepared with acceptable radiochemical purity and specific activities. Stability and partition coefficient of the complexes were determined in the final formulations and biodistribution studies in mouse demonstrated high accumulation of [¹⁶⁶Ho]–TDMPP in the lung and liver and less excretion through the kidney. while [¹⁶⁶Ho]–TTMPP was mostly excreted into intestines and kidneys while lungs were a minor accumulation site. In contrast to other reported radiolanthanide labeled porphyrins these two complexes showed less liver accumulation. Further investigation of their potential therapeutic properties is of interest.