Home
Resources
Publications
Sulfoximines as ATR Inhibitors: Analogs of VE-821

Sulfoximines as ATR Inhibitors: Analogs of VE-821

Christine M M Hendriks, Jörg Hartkamp, Stefan Wiezorek, Anne-Dorothee Steinkamp, Giulia Rossetti, Bernhard Lüscher, Carsten Bolm

Bioorg Med Chem Lett. 2017 Jun 15;27(12):2659-2662.

PMID: 28479198

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.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP1232410499	VE-821		1232410-49-9	Price

As a specialist in analytical chemical Products, Alfa Chemistry offers consumers a wealth of raw materials and a full range of technologies and services.

QUICK LINKS

HEADQUARTERS

Tel:

Fax:

Email: