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Design, synthesis and in vitro cytotoxicity studies of novel ?-carbolinium bromides.

ABSTRACT: A series of novel ?-carbolinium bromides has been synthesized from easily accessible ?-carbolines and 1-aryl-2-bromoethanones. The newly synthesized compounds were evaluated for their in vitro anticancer activity. Among the synthesized derivatives, compounds 16l, 16o and 16s exhibited potent anticancer activity with IC50 values of <10?M against tested cancer cell lines. The most potent analogue 16l was broadly active against all the tested cancer cell lines (IC50=3.16-7.93?M). In order to test the mechanism of cell death, we exposed castration resistant prostate cancer cell line (C4-2) to compounds 16l and 16s, which resulted in increased levels of cleaved PARP1 and AO/EB staining, indicating that ?-carbolinium salts induce apoptosis in these cells. Additionally, the most potent ?-carbolines 16l and 16s were found to inhibit tubulin polymerization.

SUBMITTER: Venkataramana Reddy PO 

PROVIDER: S-EPMC6368682 | biostudies-literature | 2017 Mar

REPOSITORIES: biostudies-literature

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Design, synthesis and in vitro cytotoxicity studies of novel β-carbolinium bromides.

Venkataramana Reddy P O PO   Mishra Shriprada S   Tantak Mukund P MP   Nikhil Kumar K   Sadana Rachna R   Shah Kavita K   Kumar Dalip D  

Bioorganic & medicinal chemistry letters 20170209 6

A series of novel β-carbolinium bromides has been synthesized from easily accessible β-carbolines and 1-aryl-2-bromoethanones. The newly synthesized compounds were evaluated for their in vitro anticancer activity. Among the synthesized derivatives, compounds 16l, 16o and 16s exhibited potent anticancer activity with IC<sub>50</sub> values of <10μM against tested cancer cell lines. The most potent analogue 16l was broadly active against all the tested cancer cell lines (IC<sub>50</sub>=3.16-7.93μ  ...[more]

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