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  • Synthesis and biological evaluation of L-cysteine derivatives as mitotic kinesin Eg5 inhibitors.

Synthesis and biological evaluation of L-cysteine derivatives as mitotic kinesin Eg5 inhibitors.

Bioorganic & medicinal chemistry letters (2007-05-26)
Naohisa Ogo, Shinya Oishi, Kenji Matsuno, Jun-ichi Sawada, Nobutaka Fujii, Akira Asai
ABSTRACT

Inhibition of Eg5 represents a novel approach for the treatment of cancer. Here, we report the synthesis and structure-activity relationship of S-trityl-L-cysteine (STLC) derivatives as Eg5 inhibitors. Some of these derivatives such as 4f demonstrated enhanced inhibitory activity against Eg5 and induced mitotic arrest with characteristic monoastral spindles in HeLa cells.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
S-Carboxymethyl-L-cysteine
Sigma-Aldrich
S-Methyl-L-cysteine, substrate for methionine sulfoxide reductase A
Sigma-Aldrich
Boc-Cys(Trt)-OH, 97%
Sigma-Aldrich
L-Cysteine, from non-animal source, BioReagent, suitable for cell culture, ≥98%
Sigma-Aldrich
L-Cysteine, BioUltra, ≥98.5% (RT)
Sigma-Aldrich
L-Cysteine, ≥97%, FG
Sigma-Aldrich
S-Benzyl-L-cysteine, 97%
SAFC
L-Cysteine
Sigma-Aldrich
Fmoc-Cys(Trt)-OH, ≥95.0% (sum of enantiomers, HPLC)
Sigma-Aldrich
L-Cysteine, 97%