- Structure-based screening and optimization of cytisine derivatives as inhibitors of the menin-MLL interaction
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The natural product-like compound 1 was identified as a direct inhibitor of the menin-MLL interaction by in silico screening. Structure-based optimization furnished analogue 1a, which showed significantly higher potency than both the lead structure 1 and the reference compound MI-2.
- Zhong, Hai-Jing,Lee, Bo Ra,Boyle, Joshua William,Wang, Wanhe,Ma, Dik-Lung,Hong Chan, Philip Wai,Leung, Chung-Hang
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supporting information
p. 5788 - 5791
(2016/05/19)
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- Highly stereoselective Friedel-Crafts alkylations of unactivated benzenes by episulfonium ion cyclizations
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Intermolecular additions of highly enantiomerically enriched episulfonium ions onto activated benzene rings are known to accomplish chiral Friedel-Crafts alkylations. Unactivated benzenes are either unreactive or can give low stereoselectivities. Intramol
- Branchaud, Bruce P,Blanchette, Heather S
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p. 351 - 353
(2007/10/03)
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- Collagen cross-links: Synthesis of pyridinoline, deoxypyridinoline and their analogues
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An efficient chiral synthesis of (S,S)-(-)-3g, a key intermediate for the preparation of collagen cross-links pyridinoline (Pyd, 1) and deoxypyridinoline (Dpd, 2) was achieved from (4S)-5(tert-butoxy)-4-[(tert- butoxycarbonyl)amino]-5-oxopentanoic acid (21b). Quaternization of (S,S)-(- )-3g with iodide (2S, 5R)-(+)-4a followed by hydrolysiS provided a first chiral synthesis of natural (+)-Pyd (1). 1-(2S)-(+)-Pyd (1) was also synthesized from (S,S)-(-)-3g and iodide (2S, 5S)-(+)-4a. Similarly, quaternization of (S,S)-(-)-3g with iodide (2S)-(-)-4b, which was prepared from (2S)-(-)-6-amino-2[(tert-butoxycarbonyl)amino]hexanoic acid (31) in three steps, followed by hydrolysis afforded natural (+)-Dpd (2) in 5.3% overall yield. Also, the synthesis of racemic Dpd [(±)-2] and a variety of its analogues is presented.
- Adamczyk, Maciej,Johnson, Donald D.,Reddy, Rajarathnam E.
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- Alpha-(phenylalkyl) pyridinealkanol derivatives
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This invention relates to novel α-(phenylalkyl) pyridinealkanol derivatives useful in the treatment of diseases or disorders mediated by platelet-activating factor. This invention further relates to pharmaceutical compositions of such α-(phenylalkyl)pyridinealkanol derivatives.
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- Certain 1H-imidazol-1-yl-1-lower-alkanoic acid derivatives having anti-thrombotic activity
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Compounds of the general formula STR1 and pharmaceutically acceptable salts thereof have antithrombotic activity. Het represents 1-[1H-imidazolyl], 1-N-morpholinyl or pyridyl. A representative compound is 6-[2-(1H-Imidazol-1-yl)-1-yl-1-[[(4-methoxyphenyl)methoxy]methyl]ethoxy]hexanoic acid.
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