Synthesis and anticancer activity studies of indolylisoxazoline analogues

Bioorg Med Chem Lett. 2018 Sep 15;28(17):2842-2845. doi: 10.1016/j.bmcl.2018.07.035.

M V S K Chaitanya ¹, P O Venkataramana Reddy ¹, Kumar Nikhil ², Anil Kumar ¹, Kavita Shah ³, Dalip Kumar ⁴

Affiliations

1 Department of Chemistry, Birla Institute of Technology and Science, Pilani 333031, Rajasthan, India.
2 Purdue University Center for Cancer Research, Purdue University, West Lafayette, IN 47907, United States.
3 Purdue University Center for Cancer Research, Purdue University, West Lafayette, IN 47907, United States. Electronic address: shah23@purdue.edu.
4 Department of Chemistry, Birla Institute of Technology and Science, Pilani 333031, Rajasthan, India. Electronic address: dalipk@pilani.bits-pilani.ac.in.

PMID: 30072225 DOI: 10.1016/j.bmcl.2018.07.035

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.

Keywords

Anticancer activity; Apoptosis; Indole heterocycles; Indolylisoxazolines; Isoxazolines.

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