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Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)
 

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Synthesis and structure-activity relationship of 2-aminobenzophenone derivatives as antimitotic agents.

A new type of inhibitor of tubulin polymerization was discovered on the basis of the combretastatin molecular skeleton. The lead compounds in this series, compounds 6 and 7, strongly inhibited tubulin polymerization in vitro and significantly arrested cells at the G(2)/M phase. Compounds 6 and 7 yielded 50- to 100-fold lower IC(50) values than did combretastatin A-4 against Colo 205, NUGC3, and HA22T human cancer cell lines as well as similar or greater growth inhibitory activities than did combretastain A-4 against DLD-1, HR, MCF-7, DU145, HONE-1, and MES-SA/DX5 human cancer cell lines. Structure-activity relationship information revealed that introduction of an amino group at the ortho position of the benzophenone ring plays an integral role for increased growth inhibition.[1]

References

  1. Synthesis and structure-activity relationship of 2-aminobenzophenone derivatives as antimitotic agents. Liou, J.P., Chang, C.W., Song, J.S., Yang, Y.N., Yeh, C.F., Tseng, H.Y., Lo, Y.K., Chang, Y.L., Chang, C.M., Hsieh, H.P. J. Med. Chem. (2002) [Pubmed]
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