Building siRNAs with Cubes: Synthesis and Evaluation of Cubane-Modified siRNAs was written by Hammill, Matthew L.; Salim, Lidya; Tsubaki, Kouta; Varley, Andrew J.; Kitamura, Mitsuru; Okauchi, Tatsuo; Desaulniers, Jean-Paul. And the article was included in ChemBioChem on October 13,2021.Safety of Cubane-1,4-diyldimethanol The following contents are mentioned in the article:
Cubane mols. hold great potential for medicinal chem. applications due to their inherent stability and low toxicity. In this study, we report the synthesis of a cubane derivative phosphoramidite for the incorporation of cubane into small interfering RNAs (siRNAs). Synthetic siRNAs rely on chem. modifications to improve their pharmacokinetic profiles. However, they are still able to mediate sequence-specific gene silencing via the endogenous RNA interference pathway. We designed a library of siRNAs bearing cubane at different positions within the sense and antisense strands. All siRNAs showed excellent gene-silencing activity, with IC50 values ranging from 45.4 to 305 pM. Incorporating the cubane modification in both the sense and antisense strand led to viable duplexes with good biol. activity. To the best of our knowledge, this is the first report of siRNAs bearing a cubane derivative within the backbone. This study involved multiple reactions and reactants, such as Cubane-1,4-diyldimethanol (cas: 60462-27-3Safety of Cubane-1,4-diyldimethanol).
Cubane-1,4-diyldimethanol (cas: 60462-27-3) belongs to alcohols. Alkyl halides are often synthesized from alcohols, in effect substituting a halogen atom for the hydroxyl group. Alcohols may be oxidized to give ketones, aldehydes, and carboxylic acids. These functional groups are useful for further reactions. Oxidation of organic compounds generally increases the number of bonds from carbon to oxygen (or another electronegative element, such as a halogen), and it may decrease the number of bonds to hydrogen.Safety of Cubane-1,4-diyldimethanol
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