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- W2276720341 abstract "Proc Amer Assoc Cancer Res, Volume 45, 20042988 Pladienolides, novel 12-membered macrolides possessing an inhibitory activity of hypoxia-induced vascular endothelial growth factor (VEGF) expression, were isolated from Streptomyces platensis Mer-11107. Some of the pladienolides have been shown to have a strong inhibitory growth activity in various cancer cell lines at nanomolar concentrations and a good in vivo antitumor activity against human tumor xenografts. Further, these macrolides appear to have a different mechanism of action from those of pre-existing anticancer agents in clinical use according to the COMPARE analysis data. In order to enhance the potency of the naturally occurring pladienolides, synthetic derivatives were prepared and evaluated. We describe herein the synthetic approach for the derivatization of pladienolide D that led us to the discovery of E7107, which has a wide tumor spectrum, a high regression rate, and a wide therapeutic window. One of our synthetic approaches was the replacement of the acetoxy group in position-7 with a urethane moiety. Urethane derivatives were synthesized from pladienolide D in 7 steps employing commonly used and simple organic reactions. The replacement of the acetoxy group with a simple urethane moiety decreased the in vitro antiproliferative activity. However, by introducing an amino function onto the urethane moiety, the activity was regained. Many of the derivatives in this series showed a strong in vitro activity as potent as pladienolide D. A correlation between the lipophilicity of these derivatives and their in vitro activity was observed. Detailed data will be presented at the meeting. In the human colon WiDr xenograft model, several of the urethane derivatives showed more potent in vivo tumor regression activity than that of pladienolide D. Among these derivatives, E7107 was found to have an impressive tumor regression activity against WiDr xenograft with a wide dose range. These results suggest that E7107 might be a promising therapeutic agent for the treatment of cancer." @default.
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- W2276720341 date "2004-04-01" @default.
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- W2276720341 title "E7107, a new 7-urethane derivative of pladienolide D: Discovery of a novel antitumor agent" @default.
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