4.5 Article

Anti-cancer activity of carbamate derivatives of melampomagnolide B

期刊

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 24, 期 15, 页码 3499-3502

出版社

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2014.05.059

关键词

Parthenolide; Melampomagnolide B; Anti-cancer activity; Carbamates; Heterocyclic amines

资金

  1. NIH/National Cancer Institute [R01 CA158275]
  2. Arkansas Research Alliance

向作者/读者索取更多资源

Melampomagnolide B (MMB) is a natural sesquiterpene structurally related to parthenolide (PTL). We have shown that MMB exhibits anti-leukemic properties similar to PTL. Unlike PTL, the presence of a primary hydroxyl group in the MMB molecule allows the opportunity for examining the biological activity of a variety of conjugated analogs of MMB. We have now synthesized a series of carbamate analogs of MMB and evaluated these derivatives for anti-cancer activity against a panel of sixty human cancer cell lines. Analogs 6a and 6e exhibited promising anti-leukemic activity against human leukemia cell line CCRF-CEM with GI(50) values of 680 and 620 nM, respectively. Analog 6a also showed GI(50) values of 1.98 and 1.38 mu M respectively, against RPMI-8226 and SR leukemia cell lines and GI(50) values of 460 and 570 nM against MDA-MB-435 melanoma and MDA-MB-468 breast cancer cell lines, respectively. Analog 6e had GI(50) values of 650 and 900 nM against HOP-92 non-small cell lung and RXF 393 renal cancer cell lines. (C) 2014 Published by Elsevier Ltd.

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