Synthesis of heteroannulated cyclopent[b]indoles: Exploration of in vitro cytotoxicity and molecular docking studies |
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| Authors: | Rajendran Satheeshkumar Aathi Muthusankar Lincy Edatt V B Sameer Kumar Hazel A Sparkes |
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| Institution: | 1. Department of Chemistry, Bharathiar University, Coimbatore, Tamil Nadu, India;2. Membrane Protein Biology Group, International Centre for Genetic Engineering and Biotechnology, New Delhi, India;3. Department of Biochemistry and Molecular Biology, Central University of Kerala, Padenakad, Kasaragod, India;4. Department of Chemistry, University of Bristol, Bristol, UK |
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| Abstract: | A series of novel cyclopentb]indole analogues that hold isoxazolo-, pyrido-templates were designed and synthesized in good yields. The in vitro cytotoxicity was concerned for all the newly synthesized compounds by MTT assay against HeLa (cervix adeno carcinoma) and MCF-7 (breast cancer). These synthesized compounds were further compared with the standard drug ellipticine, 5-fluorouracil, cisplatin, and methotrexate. The synthesized heteroannulated cyclopentb]indole compounds were found to show better cytotoxic activity against HeLa and MCF-7 with primary structure activity relationship studies. To identify with the nature of interactions of these molecules, we performed molecular docking studies using the protein kinase CK2 inhibitors. The docking results afforded some valuable information for the future design of more potent inhibitors. |
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| Keywords: | CK2 inhibitors HeLa and MCF-7 isoxazolo-cyclopent[b]indole pyrido-cyclopent[b]indole |
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