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Updated: Jul 16, 2026

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
Syntheses and antiproliferative evaluation of oxyphenisatin derivatives
Muhammed K Uddin1, Serge G Reignier, Tom Coulter
1Evotec(UK) Ltd, 111 Milton Park, Abingdon, Oxon OX14 4RX, UK.
Abstract:
Syntheses and structure-antiproliferative relationship for oxyphenisatin analogues are described. The cell proliferation data showed that the presence of substituents (especially F, Cl, Me, CF(3), and OMe) in the 6- and 7-position of oxyphenisatin markedly enhanced the potency in the MDA-468 cell line without affecting the MDA-231 cell line. The best compounds from this series showed low nanomolar antiproliferative activity towards the MDA-468 cell line and a 1000-fold selectivity over the MDA-231 cell line.
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