Colchicine-like β-acetamidoketones as inhibitors of microtubule polymerization: Design, synthesis and biological evaluation of in vitro anticancer activity

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Karimikia Ehsan; BEHRAVAN JAVAD; ZARGHI AFSHIN; GHANDADI MORTEZA; OMID MALAYERI SINA; GHODSI RAZIEH

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Journal Paper

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Journal: Iranian Journal of Basic Medical Sciences Year:2019 | Volume:22 | Issue:10 Page(s): 1138-1146

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Title

Colchicine-like β-acetamidoketones as inhibitors of microtubule polymerization: Design, synthesis and biological evaluation of in vitro anticancer activity

Author(s)

Keywords

Anticancer activity

Chalcone

Colchicine

Colchicine–

like

Molecular docking

Tubulin polymerization

-acetamidoketones

Abstract

Objective(s): In this study a series of novel Colchicine-like β;-acetamidoketones was designed and synthesized as potential tubulin inhibitors Materials and Methods: The cytotoxicity of the novel synthesized β;-acetamidoketones was assessed against two cancerous cell lines including MCF-7 (human breast cancer cells) and A549 (adenocarcinomic human alveolar basal epithelial cells) employing the MTT test. Tubulin polymerization test was done by using a commercial kit (Tubulin polymerization assay kit). Results: In general, the cytotoxicity activities were highly dependent on the aromatic substitution pattern of phenyl ring at β; position of β;-acetamidoketones. Based upon, compound 4f possessing the same structural elements of Colchicine and Chalcone 1, revealed the most cytotoxicity more than the other β;-acetamidoketone against the cancerous cell lines and showed moderate antitubulin effect. The tubulin inhibitory effect of 4f, Colchicine and Chalcone 1 were consistent with their antiproliferative activities. Molecular docking studies of 4f, into the Colchicine-binding site of tubulin exhibited possible mode of interaction between this compound and tubulin. Conclusion: The structure activity relationship (SAR) data attained showed that the presence of trimethoxy phenyl attached to carbonyl group of β;-acetamidoketones and a methoxy group at para position of the other ring are essential for cytotoxic activity. In general, the cytotoxicity activities were highly dependent on the aromatic substitution pattern of phenyl ring at β; position of β;-acetamidoketones.

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APA: Copy

Karimikia, Ehsan, BEHRAVAN, JAVAD, ZARGHI, AFSHIN, GHANDADI, MORTEZA, OMID MALAYERI, SINA, & GHODSI, RAZIEH. (2019). Colchicine-like β-acetamidoketones as inhibitors of microtubule polymerization: Design, synthesis and biological evaluation of in vitro anticancer activity. IRANIAN JOURNAL OF BASIC MEDICAL SCIENCES, 22(10), 1138-1146. SID. https://sid.ir/paper/724442/en

Vancouver: Copy

Karimikia Ehsan, BEHRAVAN JAVAD, ZARGHI AFSHIN, GHANDADI MORTEZA, OMID MALAYERI SINA, GHODSI RAZIEH. Colchicine-like β-acetamidoketones as inhibitors of microtubule polymerization: Design, synthesis and biological evaluation of in vitro anticancer activity. IRANIAN JOURNAL OF BASIC MEDICAL SCIENCES[Internet]. 2019;22(10):1138-1146. Available from: https://sid.ir/paper/724442/en

IEEE: Copy

Ehsan Karimikia, JAVAD BEHRAVAN, AFSHIN ZARGHI, MORTEZA GHANDADI, SINA OMID MALAYERI, and RAZIEH GHODSI, “Colchicine-like β-acetamidoketones as inhibitors of microtubule polymerization: Design, synthesis and biological evaluation of in vitro anticancer activity,” IRANIAN JOURNAL OF BASIC MEDICAL SCIENCES, vol. 22, no. 10, pp. 1138–1146, 2019, [Online]. Available: https://sid.ir/paper/724442/en

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