Synthesis of exotic polycycles such as cyclooctatrienes and fenestrenes with differential pro-apoptotic activities on human TRAIL-resistant metastatic cell lines
✍ Scribed by Catherine Hulot; Jean Peluso; Gaëlle Blond; Christian D. Muller; Jean Suffert
- Book ID
- 104004815
- Publisher
- Elsevier Science
- Year
- 2010
- Tongue
- English
- Weight
- 304 KB
- Volume
- 20
- Category
- Article
- ISSN
- 0960-894X
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✦ Synopsis
a b s t r a c t New cyclooctatrienes were prepared by semihydrogenation of trienynes followed by 8p electrocyclization. Cyclooctatrienes and original fenestrenes previously reported were tested for their pro-apoptotic activities on two human cancer cell lines (THP-1 and SW620). Among the 20 new compounds tested, two compounds presented specific activities on the colon carcinomas TRAIL-resistant metastatic cell SW620, but a minor action on the monocytic leukemia THP-1 cell line. Six other compounds showed cell type specific activities: four induced apoptosis only in THP-1 cells and two only in SW620. Such differential pro-apoptotic activities suggest that these molecules could serve as potent pharmacological tools to study TRAIL associated cellular mechanisms.