TY  - JOUR
AU  - Hendriks, Christine M. M.
AU  - Hartkamp, Jörg
AU  - Wiezorek, Stefan
AU  - Steinkamp, Anne-Dorothee
AU  - Rossetti, Giulia
AU  - Lüscher, Bernhard
AU  - Bolm, Carsten
TI  - Sulfoximines as ATR inhibitors: Analogs of VE-821
JO  - Bioorganic & medicinal chemistry letters
VL  - 27
IS  - 12
SN  - 0960-894X
CY  - Amsterdam [u.a.]
PB  - Elsevier Science
M1  - FZJ-2017-04039
SP  - 2659 - 2662
PY  - 2017
AB  - The ATM- and Rad3-related (ATR) kinases play a key role in DNA repair processes and thus ATR is an attractive target for cancer therapy. Here we designed and synthesized sulfilimidoyl- and sulfoximidoyl-substituted analogs of the sulfone VE-821, a reported ATR inhibitor. The properties of these analogs have been investigated by calculating physicochemical parameters and studying their potential to specifically inhibit ATR in cells. Prolonged inhibition of ATR by the analogs in a Burkitt lymphoma cell line resulted in enhanced DNA damage and a substantial amount of apoptosis. Together our findings suggest that the sulfilimidoyl- and sulfoximidoyl-substituted analogs are efficient ATR inhibitors.
LB  - PUB:(DE-HGF)16
UR  - <Go to ISI:>//WOS:000402472600004
DO  - DOI:10.1016/j.bmcl.2017.04.026
UR  - https://juser.fz-juelich.de/record/830498
ER  -