83553-49-5Relevant articles and documents
A concise and efficient route to the total synthesis of bacillamide A and its analogues
Kumar, Sunil,Aggarwal, Ranjana
, p. 354 - 361 (2018/07/05)
The synthesis of bacillamide A, a tryptamide alkaloid of marine origin, and its analogues from L-cysteine ethyl ester hydrochloride through an efficient and convergent synthetic approach is described in this work. The present two-step protocol involves th
Synthesis and Biological Investigation of Oxazole Hydroxamates as Highly Selective Histone Deacetylase 6 (HDAC6) Inhibitors
Senger, Johanna,Melesina, Jelena,Marek, Martin,Romier, Christophe,Oehme, Ina,Witt, Olaf,Sippl, Wolfgang,Jung, Manfred
supporting information, p. 1545 - 1555 (2016/03/08)
Histone deacetylase 6 (HDAC6) catalyzes the removal of an acetyl group from lysine residues of several non-histone proteins. Here we report the preparation of thiazole-, oxazole-, and oxadiazole-containing biarylhydroxamic acids by a short synthetic proce
A catch-and-release strategy for the combinatorial synthesis of 4-acylamino-1,3-thiazoles as potential CDK5 inhibitors
Larsen, Scott D.,Stachew, Carl F.,Clare, Paula M.,Cubbage, Jerry W.,Leach, Karen L.
, p. 3491 - 3495 (2007/10/03)
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.