- Five-membered heterocyclic ureas suitable for the donor-donor-acceptor hydrogen-bonding modules
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Five-membered heterocyclic ureas are capable of forming the unfolded conformer without preorganization by using the intramolecular hydrogen bond, and are suitable for the DDA hydrogen-bonding modules. In contrast, six-membered heterocyclic ureas are desta
- Hisamatsu, Yosuke,Fukumi, Yuki,Shirai, Naohiro,Ikeda, Shin-ichi,Odashima, Kazunori
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p. 2005 - 2009
(2008/09/19)
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- A catch-and-release strategy for the combinatorial synthesis of 4-acylamino-1,3-thiazoles as potential CDK5 inhibitors
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Two-dimensional libraries of 4-acylamino-1,3-thiazoles 9 were prepared via Curtius rearrangement of 1,3-thiazole-4-carbonyl azides 6, trapping of the intermediate isocyanates with oxime resin, and thermal regeneration of the isocyanates from the washed resin in the presence of nucleophiles. Several compounds proved to be selective inhibitors of CDK5/p25 versus the closely homologous CDK2/cyclin A enzyme, with the best analogue (43) possessing over 100-fold selectivity.
- Larsen, Scott D.,Stachew, Carl F.,Clare, Paula M.,Cubbage, Jerry W.,Leach, Karen L.
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p. 3491 - 3495
(2007/10/03)
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