| 2 | Author
| FrankI. Bohnenstengel3, KlausG. Steubeb, CorinnaM. Eyerb, BambangW. Nugroho3, PhamD. Hungc, LeC. Kietd, Peter Proksch3 | Requires cookie* | | Title
| Structure Activity Relationships of Antiproliferative Rocaglamide Derivatives from Aglaia Species (Meliaceae)  | | | Abstract
| Eleven rocaglamide derivatives (cyclopentatetrahydrobenzofurans) and one structurally related aglain congener all isolated from different Aglaia species (Meliaceae) were tested for growth inhibiting properties using the human cancer cell lines MONO-MAC-6 and MEL-JUSO. Proliferation of both cell lines was efficiently inhibited in a dose and compound de pendent manner. Applying a MTT-Assay, the IC50 of the most active compound didesmethyl-rocaglamide (1) was observed at 0.002 and 0.006 [ig/ml (0.004 and 0.013 j.iM) depending on the cell line investigated. Bulky aminoacyl substituents at C-2, acetylation of the OH substitu ent at C-l or insertion of a OH or OMe substituent at C-3 of the rocaglamide skeleton all diminished the activity of the compounds investigated. The aglain derivative 12 was inactive up to a concentration of 3 ng/ml (4.6 [ . i m) . This loss of activity is assumed to be mainly due to the presence of a pyran ring in the aglains vs. a furan ring as found in rocaglamide derivatives. Rocaglamide derivatives may act primarily by inhibition of cell proliferation as evidenced by the absence of a significant cytotoxic effect in long-term cultures of MONO-MAC-6 cells treated with high doses of didesmethylrocaglamide. O ur data suggest that rocaglamide derivatives could exert a potential role in the treatm ent of malignant diseases and are worth to be investigated in further studies of experimental medicine and pharmacology. | | |
Reference
| Z. Naturforsch. 54c, 55—6 (1999); received September 28/October 21 1998 | | |
Published
| 1999 | | |
Keywords
| Aglaia spp, Meliaceae, Rocaglamide, Cyclopentatetrahydrobenzofurans, Antiproliferative Activity, Cancer Cells, M ONO-M AC-6 | | |
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| ZNC-1999-54c-0055 | | | Volume
| 54 | |
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