46(P-7) 新規M期作用薬MPC1001および同族体の構造(ポスター発表の部)

概要

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In the course of our search for new antimitotic antitumor agents from microbial source, the fungus Cladorrhinum sp. KY4922 strain was found to produce a series of new compounds. Eight new compounds, MPC1001 (1), and MPC1001B (2)〜MPC1001H (8) were isolated from the culture broth by column chromatographies with various separation modes. The molecular formula of 1 was determined to be C_<28>H_<24>N_2O_<10>S_2 by HR-FAB MS and ^<13>C-NMR spectra. Interpretations of 1D and 2D NMR spectra along with physico-chemical data, 1 was revealed to be a new methyl derivative of emestrin, 15-membered antifungal macrolide possessing a unique epidithiodioxopiperazine moiety. The relative configuration of 1 elucidated by proton coupling constants and NOE experiments and the absolute structure via CD spectrum were the same as emestrin. 2 and 3 were deoxy, and 4 was trisulfide analogs of 1. Moreover, 5〜8 were retro-aldol type seco-aldehydes. 1 had an ability to arrest HCT 116 human colon cancer cells at M phase and exhibited an antiproliferative activity with the IC_<50> value 3.3nM. Other analogs possessing the polysulfide bridge also exerted potent antiproliferative activities against human prostate cancer cell line DU145.
天然有機化合物討論会の論文
2003-09-01