期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 58, 期 22, 页码 8896-8906出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.jmedchem.5b01187
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资金
- NIH/National Cancer Institute [R01 CA158275]
- NIH/National Institute of General Medical Sciences [P20GM109005]
- UAMS Translational Research Institute (TRI) through NIH National Center for Research Resources [UL1TR000039]
- National Center for Advancing Translational Sciences
- UAMS Department of Radiology
- Office Of The Director
- Office of Integrative Activities [1457888] Funding Source: National Science Foundation
Novel carbamate (7a-7h) and carbonate (7i, 7j, and 8) dimers of melampomagnolide B have been synthesized by reaction of the melampomagnolide-B-triazole carbamate synthon 6 with various terminal diamino- and dihydroxyalkanes. Dimeric carbamate products 7b, 7c, and 7f exhibited potent growth inhibition (GI(50) = 0.16-0.99 mu M) against the majority of cell lines in the NCI panel of 60 human hematological and solid tumor cell lines. Compound 7f and 8 exhibited anticancer activity that was 300-fold and 1 x 10(6)-fold more cytotoxic that DMAPT, respectively, at a concentration of 10 mu M against rat 9L-SF gliosarcoma cells. Compounds 7a-7j and 8 were also screened against M9-ENL1 and acute myelogeous leukemia (AML) primary cell lines and exhibited 2- to 10-fold more potent antileukemic activity against M9-ENL1 cells (EC50 = 0.57-2.90 mu M) when compared to parthenolide (EC50 = 6.0) and showed potent antileukemic activity against five primary AML cell lines (EC50 = 0.76-7.3 mu M).
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