Journal
ACS MEDICINAL CHEMISTRY LETTERS
Volume 5, Issue 1, Pages 94-97Publisher
AMER CHEMICAL SOC
DOI: 10.1021/ml400457j
Keywords
Retro-2.1; Shiga toxin; ricin; dihydroquinazolinones
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Funding
- French National Agency for Research (ANR) [ANR-11-BSV2-0018]
- Joint ministerial program of R&D against CBRNe risks
- CEA
- CEA international PhD program
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This study reports the synthesis, chromatographic separation, and pharmacological evaluation of the two enantiomers of a new compound, named Retro-2.1, active against toxins by inhibiting intracellular trafficking via the retrograde route. The absolute configuration of the bioactive enantiomer has been assigned from X-ray diffraction to the (S)-enantiomer. To date, (S)-Retro-2.1 is the most potent molecule to counteract the cytotoxic potential of ricin and Shiga toxin, with EC50 values of 23 and 54 nM, respectively.
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