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Large-scale synthesis of GMP grade alpha-cyano-beta-hydroxy-beta-methyl-N-(2,5-dibromophenyl) propenamide (LFM-A13), a new anti-cancer drug candidate.

作者信息

DuMez Darin, Venkatachalam Taracad K, Uckun Fatih M

机构信息

Paradigm Pharmaceuticals, 2139 Fourth Street, White Bear Lake, MN 55110, USA.

出版信息

Arzneimittelforschung. 2007;57(3):155-63. doi: 10.1055/s-0031-1296599.

Abstract

The leflunomide (CAS 75706-12-6) metabolite (LFM) analog alpha-cyano-beta-hydroxy-beta-methyl-N-(2,5-dibromophenyl)-propenamide (LFM-A13, DDE-28, CAS 244240-24-2), is a rationally designed inhibitor of the anti-apoptotic enzyme Bruton's tyrosine kinase (BTK). LFM-A13 is being developed as a novel dual-function anticancer drug with apoptosis-promoting and anti-thrombotic properties. LFM-A13 was prepared under current Good Manufacturing Practice (cGMP) conditions on the scale of kilograms.

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