A new class of isobenzofuran-5-carboxamide derivatives: synthesis, studies on induction of apoptosis and inhibition of cancer cell proliferation

Ningegowda, Raghu and Swamy, Nanjunda S and Achar, Raghu Ram and Basappa, . and Gaonkar, Santosh L and Ranjith, S and George, Yip W and Priya, B S (2015) A new class of isobenzofuran-5-carboxamide derivatives: synthesis, studies on induction of apoptosis and inhibition of cancer cell proliferation. Asian Journal of Biochemical and Pharmaceutical Research, 5 (2). pp. 2231-2560. ISSN 2231-2560

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Abstract

Keeping in view that carboxamides have a wide array of biological activities, 1-(4-fluorophenyl)- 1,3 dihydroisobenzofuran-5-carboxylic acid was coupled with aromatic and aliphatic amines to obtain a new series of isobenzofuran-5-carboxamide derivatives. These derivatives were analyzed for their antiproliferative efficacy against human breast cancer cells and prostate cancer cells. All the compounds showed antiproliferative activity against LNCaP prostate cancer cell lines. The compound 4b showed antiproliferative activity against MDA-MB 231 (IC50 =40±1.1 μM), MCF-7(IC50 =36±1.4μM), PC3 (IC50=42±1.7 μM ) and LNCaP (IC50 =20±1.1 μM ) cancer cells. Compound 4b showing a promising antiproliferative effect induced apoptosis in LNCaP prostate cancer cells. In-silico molecular docking reveals the interaction of the 4b with caspase 7. Additionally, the in-silico pharmacokinetic parameters reflect the drug like properties of the all the synthesized isobenzofuran carboxamides

Item Type: Article
Uncontrolled Keywords: isobenzofuran carboxamides, antiproliferative activity, in silico molecular docking, caspase 3/7
Subjects: Engineering > MIT Manipal > Chemistry
Depositing User: MIT Library
Date Deposited: 19 Dec 2015 16:10
Last Modified: 19 Dec 2015 16:10
URI: http://eprints.manipal.edu/id/eprint/144855

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