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Synthesis and biological studies of new piperidino-1,2,3-triazole hybrids with 3-aryl isoxazole side chains

Abstract : A small library of new piperidine-triazole hybrids with 3-aryl isoxazole side chains has been designed and synthesized. Their cytotoxicity against a panel of seven cancer cell lines has been established. For the most promising compound, an IC(50) value of 3.8 μM on PUMA/Bcl-xL interaction in live cancer cells was established through BRET analysis. A rationale was proposed for these results through complete molecular modelling studies.
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https://hal.archives-ouvertes.fr/hal-03414697
Contributor : Laurent Jonchère Connect in order to contact the contributor
Submitted on : Wednesday, November 10, 2021 - 2:17:21 PM
Last modification on : Friday, May 13, 2022 - 4:09:20 PM
Long-term archiving on: : Friday, February 11, 2022 - 6:58:26 PM

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Distributed under a Creative Commons Attribution - NonCommercial 4.0 International License

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Appala Venkata Ramana Murthy, Vennu Narendar, Nangunoori Sampath Kumar, Pasula Aparna, Anagani Kanaka Durga Bhavani, et al.. Synthesis and biological studies of new piperidino-1,2,3-triazole hybrids with 3-aryl isoxazole side chains. Bioorganic & Medicinal Chemistry Letters, 2021, 52, pp.128390. ⟨10.1016/j.bmcl.2021.128390⟩. ⟨hal-03414697⟩

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