- The 1,4-benzodiazepine-2,5-dione small molecule template results in melanocortin receptor agonists with nanomolar potencies
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The melanocortin system consists of five seven-transmembrane spanning G-protein coupled receptors (MC1-5) that are stimulated by endogenous agonists and antagonized by the only two known endogenous antagonists of GPCRs, agouti and agouti-related protein (
- Joseph, Christine G.,Wilson, Krista R.,Wood, Michael S.,Sorenson, Nicholas B.,Phan, Dong V.,Xiang, Zhimin,Witek, Rachel M.,Haskell-Luevano, Carrie
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p. 1423 - 1431
(2008/09/21)
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- A novel solid-phase synthetic method for 1,4-benzodiazepine-2,5-dione derivatives
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Utilizing polymer-bound anthranilic acid derivatives 1, we were able to obtain the 1,4-benzodiazepine-2,5-dione derivatives 3 (R3 = H, R 4 = H, MeO, Cl) through an unprecedented reaction sequence, reductive alkylation-N-protected amino acid coupling-deprotective cyclization, in 28-71% five-step overall isolated yields and 95-99% purities from Wang resin 4. Applying the novel protocol to the resin 2, the 7-benzamido-1,4-benzodiazepine- 2,5-dione derivatives 3 (R1 = Bn, R4 = 7-BzNH) could be obtained in 19-42% seven- or eight-step overall isolated yields and 92-98% purities from AMEBA resin 7. Thieme Stuttgart.
- Jeon, Moon-Kook,Kwon, Jeong-Jin,Kim, Myung-Su,Gong, Young-Dae
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experimental part
p. 1651 - 1656
(2009/04/07)
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- Design, synthesis and biological evaluation of 1,4-benzodiazepine-2,5-dione-based HDAC inhibitors
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New histone deacetylase inhibitors have been synthesized and evaluated for their activity against non-small lung cancer cell line H661. These compounds have been designed with diversely substituted 1,4-benzodiazepine-2,5-dione moieties as cyclic peptide m
- Loudni, Lynda,Roche, Joelle,Potiron, Vincent,Clarhaut, Jonathan,Bachmann, Christian,Gesson, Jean-Pierre,Tranoy-Opalinski, Isabelle
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p. 4819 - 4823
(2008/09/17)
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