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Synthesis and anticancer activity studies of indolylisoxazoline analogues.


ABSTRACT: A new library of thirteen indolylisoxazolines 6a-m has been synthesized by the treatment of indolylchalcones with hydroxylamine hydrochloride. Evaluation of anticancer activity of indolylisoxazolines 6a-m led to the identification of potent compounds 6c-d, 6i and 6l, with IC50 ranging 2.5-5.0 µM against the tested cancer cell lines. Using a number of complementary techniques such as acridine orange/ethidium bromide staining, PARP1 cleavage and DNA strand breaks assay, we show that the compounds 6c and 6i induce apoptosis in highly aggressive C4-2 cells. Our data further revealed that 6c and 6i inhibited C4-2 cells proliferation without inducing reactive oxygen species (ROS). Finally, we show that compounds 6c and 6i also potently inhibit cell migration, indicating these compounds have the potential to serve as effective anti-cancer agents.

SUBMITTER: Chaitanya MVSK 

PROVIDER: S-EPMC8653574 | biostudies-literature | 2018 Sep

REPOSITORIES: biostudies-literature

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Synthesis and anticancer activity studies of indolylisoxazoline analogues.

Chaitanya M V S K MVSK   Reddy P O Venkataramana POV   Nikhil Kumar K   Kumar Anil A   Shah Kavita K   Kumar Dalip D  

Bioorganic & medicinal chemistry letters 20180726 17


A new library of thirteen indolylisoxazolines 6a-m has been synthesized by the treatment of indolylchalcones with hydroxylamine hydrochloride. Evaluation of anticancer activity of indolylisoxazolines 6a-m led to the identification of potent compounds 6c-d, 6i and 6l, with IC<sub>50</sub> ranging 2.5-5.0 µM against the tested cancer cell lines. Using a number of complementary techniques such as acridine orange/ethidium bromide staining, PARP1 cleavage and DNA strand breaks assay, we show that the  ...[more]

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