Sert, Mustafa; Isilar, Ozer; Yaglioglu, Ayse Sahin; Bulut, Adnan published the artcile< Gabriel-Cromwell aziridination of amino sugars; chiral ferrocenoyl-aziridinyl sugar synthesis and their biological evaluation>, Reference of 4064-06-6, the main research area is prostate cancer therapy prodrug aziridine sugar pharmacokinetic; human antitumor Gabriel Cromwell aziridination aminosugar; Amino sugar; Aziridine; Drug likeness; Ferrocene; HeLa; PC3.
N-sugar substituted chiral aziridines were synthesized via Gabriel-Cromwell reaction. Novel pure diastereomers of aziridine derivatives (4 diastereomers) were readily obtained in high yields and their structures were confirmed by means of 1H NMR, 13C NMR, FT-IR, Mass and optical rotations. This is, to the best of our knowledge, the unique example of N-sugar aziridine synthesis. Diastereomeric effects for prostate (PC3) and cervix (HeLa) cancers were screened and it has been observed that the epimers bearing the same sugars showed different results against PC3 and HeLa cancer cells. The novel sugar aziridines were investigated as promising prodrug candidates for prostate cancer (PC3) therapy. Moreover, the drug likeness calculations (Lipinski’s rule, physicochem. properties, lipophilicity, solubility, pharmacokinetics and bioavailability radar) have indicated that the sugar aziridines can be good candidates as oral drugs.
Carbohydrate Research published new progress about Amination. 4064-06-6 belongs to class alcohols-buliding-blocks, and the molecular formula is C12H20O6, Reference of 4064-06-6.
Referemce:
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