Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10594681 | Bioorganic & Medicinal Chemistry Letters | 2012 | 7 Pages |
Abstract
A series of Pictet-Spengler condensation derivatives (tetrahydro-β-carbolines) was designed, synthesized and evaluated for lethality against a panel of seven cancer cell lines. Seven compounds (2a, 13, 20, 21, 27, 29 and 34) showed lethality in at least five cell lines. Among these, compound 27 showed a unique selectivity towards oncogenic-RAS expressing BJ-TERT/LT/ST/RASV12 tumor cells, compared to non-transformed BJ-TERT cells. Further investigation revealed that 27 induces cell death without activation of caspases. This represents a useful new probe of non-apoptotic cell death and oncogenic-RAS synthetic lethality.
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Chemistry
Organic Chemistry
Authors
Rachid Skouta, Miki Hayano, Kenichi Shimada, Brent R. Stockwell,