Bioorganic & Medicinal Chemistry Letters 2007-07-15

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

Naohisa Ogo, Shinya Oishi, Kenji Matsuno, Jun-ichi Sawada, Nobutaka Fujii, Akira Asai

文献索引：Bioorg. Med. Chem. Lett. 17 , 3921-4, (2007)

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摘要

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.

相关化合物

  • L-半胱氨酸
  • 羧甲司坦
  • S-甲基-L-半胱氨酸
  • Fmoc-S-三苯甲基-L...
  • N-叔丁氧羰基-S-三...
  • S-苄基-L-半胱氨酸

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