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Proapoptotic and anti-angiogenic activity of (2E)-3-(2-bromo-6-hydroxy-4-methoxyphenyl)-1-(naphthalene-2-yl) prop-2-en-1-one in MCF7 cell line

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In the present study, synthesized the d1 by the Claisen–Schmidt condensation method and the resultant compound was characterized by 1H NMR and 13C NMR spectral studies. Compound d1 exhibits incredible anticancer movement on MCF7 with the IC50 estimations of 6.555–10.14 µM. The further apoptotic-related examination has been finished for the expression level of Caspase 9 and Caspase 3. Supporting this, we overview the in vivo adversary of tumor development and anti-angiogenic action of d1 in Ehrlich Ascites Carcinoma (EAC). The d1 treatment inhibited the tumor development and expanded the life expectancy of the EAC-bearing mice without appearing symptoms on healthy mice, as uncovered by histological parameters. The apoptosis induced in the early apoptotic phase and Caspase activation at a specified concentration showed significant apoptotic activity. In vivo models in EAC for anti-angiogenic models also showed promising activity at a specified concentration. The present study revealed that the d1 showed significant tumor-inhibiting capabilities even in lesser concentrations in both in vitro as well as in vivo suggested that our d1 as a potent anticancer drug.

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This study was supported and funded by Rajiv Gandhi National Fellowship (RGNF-UGC); ORDER NO. SPC/43/RGNF/2013-14. P.G. Department of Biotechnology Teresian College, Mysuru; and the Department of the chemistry University of Mysore. The authors acknowledge the Teresian Research Foundation and P.G. Department of Biotechnology, Teresian College (affiliated to the University of Mysore) for providing animal cell culture facility. The authors would like to thank the Department of Pharmacy, Bharathi College of Pharmacy, KM Doddi, Mandya, and Karnataka for providing the animal house facility.

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The biological activity, synthesis, and characterizations were carried out by DKMG. The research supervisor is SJ.

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Correspondence to Shankar Jayarama.

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The authors reported no potential conflict of interest.

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Guruswamy, D.K.M., Jayarama, S. Proapoptotic and anti-angiogenic activity of (2E)-3-(2-bromo-6-hydroxy-4-methoxyphenyl)-1-(naphthalene-2-yl) prop-2-en-1-one in MCF7 cell line. Chem. Pap. 74, 2229–2237 (2020).

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