88991-21-3Relevant articles and documents
Synthesis of new simplified hemiasterlin derivatives with α,β-unsaturated carbonyl moiety
The, Chinh Pham,Thi, Tuyet Anh Dang,Hoang, Thi Phuong,Ngo, Quoc Anh,Doan, Duy Tien,Thi, Thu Ha Nguyen,Thi, Tham Pham,Thi, Thu Ha Vu,Jean,Van De Weghe,Van, Tuyen Nguyen
, p. 2244 - 2246 (2014)
In this Letter, we report a convenient and efficient method for the synthesis of new simplified derivatives of hemiasterlin in which the α,α-dimethylbenzylic moiety A is replaced by α,β- unsaturated aryl groups as Michael acceptor. Most of these derivatives have a strong cytotoxic activity on three human tumor cell lines (KB, Hep-G2 and MCF7). Analogs 17b and 17f showed a high cytotoxicity against KB and Hep-G2 cancer cell lines comparable to paclitaxel and ellipticine.
UNUSUAL AMINO ACIDS. IV. ASYMMETRIC SYNTHESIS OF THIENYLALANINES
Doebler, Christian,Kreuzfeld, H.-J.,Krause, H. W.,Michalik, M.
, p. 1833 - 1842 (2007/10/02)
(Z)-2-N-Acylamino-3-thienyl-acrylic acids and thei esters were prepared by known procedures and hydrogenated to the corresponding optically active 2-N-acetyl(or benzoyl)-3-(2- or 3-thienyl)-alanines with optically yields up to 90percent using the rhodium complexes of 'PROPRAPHOS" 6a,b and O,N-bis(diphenylphosphino)-2-exo-hydroxy,3-endo-methylamino-norbornane 6c as chiral catalysts.Recrystallization and deacylation of the obtained amino acid derivatives yields the optically pure hydrochlorides of the thienylalanines as the free amino acids.
