Journal Article

FZJ-2017-04039

http://join2-wiki.gsi.de/foswiki/pub/Main/Artwork/join2_logo100x88.png Sulfoximines as ATR inhibitors: Analogs of VE-821

Hendriks, C. M. M. ; Hartkamp, J. ; Wiezorek, S. ; Steinkamp, A.-D. ; Rossetti, G.FZJ* ; Lüscher, B. ; Bolm, C. (Corresponding author)

2017
Elsevier Science Amsterdam [u.a.]

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Please use a persistent id in citations: doi:10.1016/j.bmcl.2017.04.026

Abstract: 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.

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Contributing Institute(s):

1. Computational Biomedicine (IAS-5)
2. Jülich Supercomputing Center (JSC)
3. Computational Biomedicine (INM-9)

Research Program(s):

1. 572 - (Dys-)function and Plasticity (POF3-572) (POF3-572)
2. 511 - Computational Science and Mathematical Methods (POF3-511) (POF3-511)

Appears in the scientific report 2017

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Database coverage:
; BIOSIS Previews ; Current Contents - Life Sciences ; Ebsco Academic Search ; IF < 5 ; JCR ; NCBI Molecular Biology Database ; Nationallizenz ; SCOPUS ; Science Citation Index ; Science Citation Index Expanded ; Thomson Reuters Master Journal List ; Web of Science Core Collection

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