Publication: Synthesis of propargylamine mycophenolate analogues and their selective cytotoxic activity towards neuroblastoma SH-SY5Y cell line
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Issued Date
2021-08-01
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ISSN
14643405
0960894X
0960894X
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2-s2.0-85107125312
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Mahidol University
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SCOPUS
Bibliographic Citation
Bioorganic and Medicinal Chemistry Letters. Vol.45, (2021)
Suggested Citation
Patamawadee Silalai, Dumnoensun Pruksakorn, Arthit Chairoungdua, Kanoknetr Suksen, Rungnapha Saeeng Synthesis of propargylamine mycophenolate analogues and their selective cytotoxic activity towards neuroblastoma SH-SY5Y cell line. Bioorganic and Medicinal Chemistry Letters. Vol.45, (2021). doi:10.1016/j.bmcl.2021.128135 Retrieved from: https://repository.li.mahidol.ac.th/handle/123456789/76095
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Title
Synthesis of propargylamine mycophenolate analogues and their selective cytotoxic activity towards neuroblastoma SH-SY5Y cell line
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Abstract
Twenty six propargylamine mycophenolate analogues were designed and synthesized from mycophenolic acid 1 employing a key step A3-coupling reaction. Their cytotoxic activity was examined against six cancer cell lines. Compounds 6a, 6j, 6t, 6u, and 6z exhibited selective cytotoxicity towards neuroblastoma (SH-SY5Y) cancer cells and were less toxic to normal cells in comparison to the lead compound, MPA 1 and a standard drug, ellipticine. Molecular docking results suggested that compound 6a is fit well in the key amino acid of three proteins (CDK9, EGFR, and VEGFR-2) as targets in cancer therapy. The propargylamine mycophenolate scaffold might be a valuable starting point for development of new neuroblastoma anticancer drugs.