Benzoyl urea derivatives that are alpha helical peptides mimetics that mimic BH3-only proteins, compositions containing them, their conjugation to cell-targeting-moieties, and their use in the regulation of cell death are disclosed. The benzoyl urea derivatives are capable of binding to and neutralizing pro-survival Bcl-2 proteins. Use of benzoyl urea derivatives in the treatment and/or prophylaxis of diseases or conditions associated with deregulation of cell death are also described.
Synthesis of Amidomethyltrifluoroborates and Their Use in Cross-Coupling Reactions
作者:Gary A. Molander、Marie-Aude Hiebel
DOI:10.1021/ol102039c
日期:2010.11.5
Amidomethyltrifluoroborates were successfully synthesized in a one-pot fashion and used in cross-coupling reactions with a wide variety of aryl and heteroaryl chlorides.
ALPHA-HELICAL MIMETICS
申请人:THE WALTER AND ELIZA HALL INSTITUTE OF MEDICAL
RESEARCH
公开号:EP1763509B1
公开(公告)日:2018-02-21
US7956216B2
申请人:——
公开号:US7956216B2
公开(公告)日:2011-06-07
A new polymer-bound N-hydroxysuccinimidyl active ester linker
作者:Hui Shao、Qiang Zhang、Robert Goodnow、Li Chen、Steve Tam
DOI:10.1016/s0040-4039(00)00619-5
日期:2000.6
Synthesis of a new N-hydroxysuccinimidyl resin is described and the N-acylation with this resin provides amide products in high yields and excellent purities. This new linker is suitable for combinatoriallibrary synthesis.