54139-51-4Relevant articles and documents
Discovery and optimization of novel benzothiophene-3-carboxamides as highly potent inhibitors of Aurora kinases A and B
Gyulavári, Pál,Szokol, Bálint,Szabadkai, István,Brauswetter, Diána,Bánhegyi, Péter,Varga, Attila,Markó, Péter,Boros, Sándor,Illyés, Eszter,Szántai-Kis, Csaba,Krekó, Marcell,Czudor, Zsófia,?rfi, László
supporting information, p. 3265 - 3270 (2018/08/24)
Aurora kinases as regulators of cell division have become promising therapeutic targets recently. Here we report novel, low molecular weight benzothiophene-3-carboxamide derivatives designed and optimized for inhibiting Aurora kinases. The most effective compound 36 inhibits Aurora kinases in vitro in the nanomolar range and diminishes HCT 116 cell viability blocking cytokinesis and inducing apoptosis. According to western blot analysis, the lead molecule inhibits Aurora kinases equipotently to VX-680 (Tozasertib) and similarly synergizes with other targeted drugs.
ACETYL FLUOROSULFONATE - GENERATION FROM ACETYL FLUORIDE AND SULFUR TRIOXIDE AND REACTIONS WITH OLEFINS
Shastin, A. V.,Balenkova, E. S.,Sorokin, V. D.,Koz'min, A. S.,Zefirov, N. S.
, p. 1039 - 1045 (2007/10/02)
The acylation of methylenecyclobutane, styrene, and vinylcyclopropane by acetyl fluorosulfonate, generated in situ from acetyl fluoride and sulfur trioxide, followed by treatment with methyl or propyl alcohols leads to the products from conjugate addition (alkoxy ketones) in addition to elimination products (α,β-unsaturated ketones).The employed methods makes it possible to separate the stages of addition of the acetyl group and the external nucleophile through the intermediate formation of covalently bonded alkyl fluorosulfonates.
