Japan
Research Article
Novel Chiral Chalcone Analogs that Induce M Phase Arrest and Apoptosis in HeLa Cells
Author(s): Weiwei Chen, Ruirong Yi, Majid Vahed, Yoshifumi Ohno, Zheng Tian, Shuhan Guo, Xue Ma, Nan Nwe Win, Qisen Li, Ayumu Tsubosaka, Kengo Saito, Shingo Nakamoto, Akiko Suganami, Yutaka Tamura, Takayoshi Arai and Hiroshi ShirasawaWeiwei Chen, Ruirong Yi, Majid Vahed, Yoshifumi Ohno, Zheng Tian, Shuhan Guo, Xue Ma, Nan Nwe Win, Qisen Li, Ayumu Tsubosaka, Kengo Saito, Shingo Nakamoto, Akiko Suganami, Yutaka Tamura, Takayoshi Arai and Hiroshi Shirasawa
We identified two chiral chalcone analogs CCL360 and CCL361 from the Chiba Chemical Library, which exhibit antiproliferative effects on human cancer cells. Flow cytometry analyses revealed that HeLa and Vero cells treated with CCL360 and CCL361 had higher populations of cells in the G2/M phase than untreated cells. Docking studies suggested that the R-isomer of CCL361 binds to the taxol binding domain (TBD) of β-tubulin, and the S-isomers of CCL360 and CCL361 bind to β-tubulin at the colchicine binding domain and the TBD. Further investigations using a fluorescent ubiquitination-based cell cycle indicator system revealed that the two compounds caused cell cycle arrest (in the M phase) and apoptosis only in HeLa cells. In non-cancerous Vero cells, however, CCL360 and CCL361 prolonged the G2/M phase without causing apoptosis. Although increased expression.. Read More»
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