Please use this identifier to cite or link to this item: https://doi.org/10.1021/jm100619x
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dc.titleSynthesis and biological evaluation of polyenylpyrrole derivatives as anticancer agents acting through caspases-dependent apoptosis
dc.contributor.authorFang, Z.
dc.contributor.authorLiao, P.-C.
dc.contributor.authorYang, Y.-L.
dc.contributor.authorYang, F.-L.
dc.contributor.authorChen, Y.-L.
dc.contributor.authorLam, Y.
dc.contributor.authorHua, K.-F.
dc.contributor.authorWu, S.-H.
dc.date.accessioned2014-10-16T08:42:56Z
dc.date.available2014-10-16T08:42:56Z
dc.date.issued2010-11-25
dc.identifier.citationFang, 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
dc.identifier.issn00222623
dc.identifier.urihttp://scholarbank.nus.edu.sg/handle/10635/95024
dc.description.abstractA 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.
dc.description.urihttp://libproxy1.nus.edu.sg/login?url=http://dx.doi.org/10.1021/jm100619x
dc.sourceScopus
dc.typeArticle
dc.contributor.departmentCHEMISTRY
dc.description.doi10.1021/jm100619x
dc.description.sourcetitleJournal of Medicinal Chemistry
dc.description.volume53
dc.description.issue22
dc.description.page7967-7978
dc.description.codenJMCMA
dc.identifier.isiut000284287200007
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