- Synthesis and kinase inhibitory activity of 3′-(S)-epi-K-252a
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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.
- Gingrich, Diane E.,Hudkins, Robert L.
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- PROCESS TO MAKE LESTAURTINIB
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A a process to make lestaurtinib, also known as (9S-(9α,10β,12α))-2,3,9,10,11,12-hexahydro- 10-hydroxy-10-(hydroxymethyl)-9-methyl-9,12-epoxy-1H-diindolo [1,2,3-fg:3',2',l'-kl]pyrrolo[3,4-i][1,6]benzodiazocin-1-one is disclosed.
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Page/Page column 5-6
(2008/12/07)
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- 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
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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
- Gingrich, Diane E.,Yang, Shi X.,Gessner, George W.,Angeles, Thelma S.,Hudkins, Robert L.
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p. 3776 - 3783
(2007/10/03)
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