97161-97-2Relevant articles and documents
Practical Preparation of K-252a from a Fermentation Solution
Kino, Mitsutaka,Shono, Kenzo,Nishimura, Tetsuo,Nagamura, Satoru
, p. 1627 - 1629 (1998)
We developed a practical preparation procedure for K-252a by methylating K-252b on an industrial scale. The water-insoluble K-252a, which was present in the cell mass, was converted to the water-soluble K-252b Na salt in an alkaline solution. The obtained K-252b was methylated with dimethylsulfate in the presence of potassium carbonate in dimethylacetamide. We have already used this method to manufacture 90 kg of K-252b from the fermentation broth, and regenerated 65 kg of K-252a from K-252b.
Synthesis, modeling, and in vitro activity of (3′S)-epi-K-252a analogues. Elucidating the stereochemical requirements of the 3′-sugar alcohol on trkA tyrosine kinase activity
Gingrich, Diane E.,Yang, Shi X.,Gessner, George W.,Angeles, Thelma S.,Hudkins, Robert L.
, p. 3776 - 3783 (2007/10/03)
Utilizing our recently published semisynthetic approach to the (3′S)-K-252a diastereomer, we report the first synthesis of the (3′R)-10 diastereomer and a set of related epimers, with the goal of defining the Stereochemical role of the 3′-sugar hydroxyl g
Synthesis and kinase inhibitory activity of 3′-(S)-epi-K-252a
Gingrich, Diane E.,Hudkins, Robert L.
, p. 2829 - 2831 (2007/10/03)
The 3′-epi diastereomer of K-252a was synthesized with the goal of evaluating the stereochemical requirements of the 3′-sugar alcohol on kinase inhibitory activity. Inverting the 3′-alcohol resulted in a 20 nM inhibitor of VEGFR2 and a 1 nM inhibitor of TrkA tyrosine kinase.
