Design and synthesis of novel 5,6-bisindolylpyrimidin-4-ones structurally related to ruboxistaurin (LY333531) |
| |
Authors: | Larry T Pierce |
| |
Institution: | Department of Chemistry, Analytical and Biological Chemistry Research Facility, Western Road, University College Cork, Cork, Ireland |
| |
Abstract: | 2,3-Bis(1-methyl-1H-indol-3-yl) methyl-3-oxopropionate is a key intermediate in the synthesis of a new family of LY333531 analogues. Base-mediated cyclocondensation with thiourea afforded novel 5,6-bis(1-methyl-1H-indol-3-yl)-2-thioxo-2,3-dihydropyrimidin-4(1H)-one, which was efficiently converted to the pyrimidin-2,4(1H,3H)-dione congener. Synthesis of a six-membered K-252c analogue, 5,6-bis(1-methyl-1H-indol-3-yl)pyrimidin-4(3H)-one, is also described. |
| |
Keywords: | Bisindolylmaleimides Bisindolylpyrimidines Uracil formation Oxidative desulfurisation Kinase inhibition |
本文献已被 ScienceDirect 等数据库收录! |
|