79653-85-3Relevant academic research and scientific papers
Structure-guided design of novel l -Cysteine derivatives as potent KSP inhibitors
Ogo, Naohisa,Ishikawa, Yoshinobu,Sawada, Jun-Ichi,Matsuno, Kenji,Hashimoto, Akihiro,Asai, Akira
, p. 1004 - 1009 (2015)
Kinesin spindle protein (KSP), known as Hs Eg5, a member of the kinesin-5 family, plays an important role in the formation and maintenance of the bipolar spindle. We previously reported S-trityl-l-cysteine derivatives as selective KSP inhibitors. Here, we report further optimizations using docking modeling in the L5 allosteric binding site, which led to the discovery of several high affinity derivatives with two fused phenyl rings in the trityl group giving low nanomolar range KSP ATPase inhibition. The representative derivatives potently inhibited cell growth of HCT116 cells in correlation with KSP inhibitory activities and significantly suppressed tumor growth in the xenograft model in vivo.
New and its salt cysteines compd.
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Paragraph 0097, (2016/12/22)
The purpose of the present invention is to provide a novel compound with Eg5 inhibiting activity that is useful as an antitumoral agent. The present invention pertains to a compound expressed by the general formula (I) (in formula (I), A represents Ch2, a
