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Polygodial and ophiobolin A analogues for covalent crosslinking of anticancer targets


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Maslivetc, V, Laguera, B, Chandra, S, Dasari, R, Olivier, WJ ORCID: 0000-0002-8838-9609, Smith, JA ORCID: 0000-0001-6313-3298, Bissember, AC ORCID: 0000-0001-5515-2878, Masi, M, Evidente, A, Mathieu, V and Kornienko, A 2021 , 'Polygodial and ophiobolin A analogues for covalent crosslinking of anticancer targets' , International Journal of Molecular Sciences, vol. 22, no. 20 , pp. 1-11 , doi: 10.3390/ijms222011256.

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In a search of small molecules active against apoptosis-resistant cancer cells, including glioma, melanoma, and non-small cell lung cancer, we previously prepared α,β- and γ,δ-unsaturated ester analogues of polygodial and ophiobolin A, compounds capable of pyrrolylation of primary amines and demonstrating double-digit micromolar antiproliferative potencies in cancer cells. In the current work, we synthesized dimeric and trimeric variants of such compounds in an effort to discover compounds that could crosslink biological primary amine containing targets. We showed that such compounds retain the pyrrolylation ability and possess enhanced single-digit micromolar potencies toward apoptosis-resistant cancer cells. Target identification studies of these interesting compounds are underway.

Item Type: Article
Authors/Creators:Maslivetc, V and Laguera, B and Chandra, S and Dasari, R and Olivier, WJ and Smith, JA and Bissember, AC and Masi, M and Evidente, A and Mathieu, V and Kornienko, A
Keywords: anticancer activity, apoptosis resistance, ophiobolin A, polygodial, Wittig reaction
Journal or Publication Title: International Journal of Molecular Sciences
Publisher: Molecular Diversity Preservation International
ISSN: 1422-0067
DOI / ID Number: 10.3390/ijms222011256
Copyright Information:

Copyright: © 2021 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons 4.0 International (CC BY 4.0) license (

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