Please use this identifier to cite or link to this item: https://doi.org/10.1021/jm100619x
Title: Synthesis and biological evaluation of polyenylpyrrole derivatives as anticancer agents acting through caspases-dependent apoptosis
Authors: Fang, Z.
Liao, P.-C.
Yang, Y.-L.
Yang, F.-L.
Chen, Y.-L.
Lam, Y. 
Hua, K.-F.
Wu, S.-H.
Issue Date: 25-Nov-2010
Source: Fang, Z., Liao, P.-C., Yang, Y.-L., Yang, F.-L., Chen, Y.-L., Lam, Y., Hua, K.-F., Wu, S.-H. (2010-11-25). Synthesis and biological evaluation of polyenylpyrrole derivatives as anticancer agents acting through caspases-dependent apoptosis. Journal of Medicinal Chemistry 53 (22) : 7967-7978. ScholarBank@NUS Repository. https://doi.org/10.1021/jm100619x
Abstract: A class of polyenylpyrroles and their analogues were designed from a hit compound identified in a fungus. The compounds synthesized were evaluated for their cell cytotoxicity against human non-small-cell lung carcinoma cell lines A549. Two compounds were found to exhibit high cytotoxicity against A549 cells with IC50 of 0.6 and 0.01 μM, respectively. The underlying mechanisms for the anticancer activity were demonstrated as caspases activation dependent apoptosis induction through loss of mitochondrial membrane potential, release of cytochrome c, increase in B-cell lymphoma-2-associated X protein (Bax) level, and decrease in B-cell lymphoma-2 (Bcl-2) level. The two compounds were nontoxic to normal human lung Beas-2b cells (IC50 > 80 μM), indicating that they are highly selective in their cytotoxicity activities. Furthermore, one compound showed in vivo anticancer activity in human-lung-cancer-cell-bearing mice. These results open promising insights on how these conjugated polyenes mediate cytotoxicity and may provide a molecular rationale for future therapeutic interventions in carcinogenesis. © 2010 American Chemical Society.
Source Title: Journal of Medicinal Chemistry
URI: http://scholarbank.nus.edu.sg/handle/10635/95024
ISSN: 00222623
DOI: 10.1021/jm100619x
Appears in Collections:Staff Publications

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