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We report the conjugation of the natural lipid squalene (SQ) with a small interfering RNA (siRNA), against the junction oncogene RET/PTC1, usually found in papillary thyroid carcinoma (PTC). The acyclic isoprenoid chain of squalene has been covalently coupled with siRNA RET/PTC1 at the 3?-terminus of the sense strand via maleimide-sulfhydryl chemistry. Remarkably, the linkage of siRNA RET/PTC1 to squalene led to an amphiphilic molecule that self-organized in H2O as siRNA-SQ RET/PTC1 nanoparticles (NPs). The siRNA-SQ RET/PTC1 NPs, stable in H2O, were used for biological studies. In vitro, they did not show any cytotoxicity. Interestingly, in vivo, on a mice xenografted RET/PTC1 experimental model, RET/PTC1-SQ NPs were found to inhibit tumor growth and RET/PTC1 oncogene and oncoprotein expression after 2.5 mg/kg cumulative dose intravenous injections. In conclusion, these results showed that the “squalenoylation” offers a new noncationic plate-form for the siRNA delivery.

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Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

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This communication describes the utility of beta-amido allylboronate as a nucleophile in the catalytic amide allylation of N-carbonyl imides. The reaction of the imide substrates with the boronates has been accomplished by using catalytic zinc bromide and basic additives (ethanol, potassium carbonate and 18-crown 6-ether), affording azaspiro-gamma-lactones through a ring opening-reclosure process with yields up to 100 %. The cost-effective and easy-to-handle method established here tolerated for gram-scale synthesis without significant loss of reaction efficiency.

Sometimes chemists are able to propose two or more mechanisms that are consistent with the available data. Application In Synthesis of Ethyl 2-amino-1H-indole-3-carboxylate, If a proposed mechanism predicts the wrong experimental rate law, however, the mechanism must be incorrect.Welcome to check out more blogs about 6433-72-3, in my other articles.

Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

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Indium-Catalyzed Amide Allylation of N-Carbonyl Imides: Formation of Azaspiro-gamma-lactones via Ring Opening-Reclosure

A novel and facile synthesis of azaspiro-gamma-lactones with a methylene-lactam framework from N-carbonyl imides is described. Mechanistic investigations provide evidence for a two-step reaction process involving ZnCl2-promoted addition of beta-amido allylindium species followed by an unexpectedly molecular-sieves-mediated ring opening-reclosure concomitantly with the loss of an N-carbonyl unit.

Because enzymes can increase reaction rates by enormous factors and tend to be very specific, Safety of Ethyl 2-amino-1H-indole-3-carboxylate, typically producing only a single product in quantitative yield, they are the focus of active research.you can also check out more blogs about 6433-72-3

Reference£º
Indole alkaloid derivatives as building blocks of natural products from?Bacillus thuringiensis?and?Bacillus velezensis?and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles