Research Papers:

Novel 3-(3, 5-difluoro-4-hydroxyphenyl)-1-(naphthalen-2-yl) prop-2-en-1-one as a potent inhibitor of MAP-kinase in HeLa cell lines and anti-angiogenic activity is mediated by HIF-1α in EAC animal model

Dileep Kumar M. Guruswamy, Kyathegowdana Doddi Srivinavasa Balaji, Kattepura Krishnappa Dharmappa and Shankar Jayarama _

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Oncotarget. 2020; 11:4661-4676. https://doi.org/10.18632/oncotarget.27836

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Dileep Kumar M. Guruswamy1, Kyathegowdana Doddi Srivinavasa Balaji1, Kattepura Krishnappa Dharmappa2 and Shankar Jayarama3

1 Department of Biotechnology, Teresian College, Siddhartha Nagara Mysore-570011, Karnataka, India

2 Department of Studies in Biochemistry, Mangalore University, Chikkaaluvara, Kodagu-571232, Karnataka, India

3 Department of Food Technology, Davanagere University, Karnataka-577002, India

Correspondence to:

Shankar Jayarama,email: [email protected]

Keywords: novel chalcone; Bcl2; caspase 3; BAX; receptor tyrosine kinase inhibitor

Received: August 25, 2020     Accepted: November 12, 2020     Published: December 15, 2020

Copyright: © 2020 Guruswamy et al. This is an open access article distributed under the terms of the Creative Commons Attribution License (CC BY 3.0), which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited.


In the present investigation, we synthesized chalcone bearing naphthalene compound d1, and on the basis of 1H-NMR, 13C NMR, and LC-MS data we had specified the structure of the synthesized compound. The resultant compound d1 was assessed for their antiproliferative action against human cancer cell lines (HeLa, HCT116, HT29, MDA-MB-231, MCF-7, and SKBR3). The IC50 range was estimated at 5.58 to 11.13 μM shows that compound d1 had remarkable anticancer activity on HeLa cell lines. Besides, it was discovered that d1 incited the mitochondrial apoptotic pathway by controlling Bax and Bcl-2 transcripts by expanding the Caspase 3 activation. We depicted the in-vivo effects of tumor advancement and the antiangiogenic activity of d1 in the EAC animal model. Tumor growth had inhibited and without symptoms the longevity of EAC containing mice expanded by the treatment of d1. Inhibition of nuclear transcriptional factor HIF-1α in EAC cells and finally it also inhibited phosphorylation of downstream signaling proteins such as ERK1/2, p38, and JNK in HeLa cells. The present investigation uncovered that d1 indicated noteworthy tumor-repressing abilities much less concentration in in-vitro and in-vivo recommended that compound d1 as the potent anticancer medication.

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