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Communication

Polygodial and Ophiobolin A Analogues for Covalent Crosslinking of Anticancer Targets

1
Department of Chemistry and Biochemistry, Texas State University, San Marcos, TX 78666, USA
2
School of Natural Sciences-Chemistry, University of Tasmania, Hobart, TAS 7001, Australia
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Dipartimento di Scienze Chimiche, Università di Napoli Federico II, Complesso Universitario Monte Sant’Angelo, Via Cintia 4, 80126 Napoli, Italy
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Department of Pharmacotherapy and Pharmaceutics, Faculté de Pharmacie, Université Libre de Bruxelles (ULB), 1050 Brussels, Belgium
5
UCRC, ULB Cancer Research Center, Université Libre de Bruxelles (ULB), 1050 Brussels, Belgium
*
Authors to whom correspondence should be addressed.
Academic Editor: Hidayat Hussain
Int. J. Mol. Sci. 2021, 22(20), 11256; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms222011256
Received: 17 September 2021 / Revised: 12 October 2021 / Accepted: 15 October 2021 / Published: 19 October 2021
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. View Full-Text
Keywords: anticancer activity; apoptosis resistance; ophiobolin A; polygodial; Wittig reaction anticancer activity; apoptosis resistance; ophiobolin A; polygodial; Wittig reaction
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MDPI and ACS Style

Maslivetc, V.; Laguera, B.; Chandra, S.; Dasari, R.; Olivier, W.J.; Smith, J.A.; Bissember, A.C.; Masi, M.; Evidente, A.; Mathieu, V.; Kornienko, A. Polygodial and Ophiobolin A Analogues for Covalent Crosslinking of Anticancer Targets. Int. J. Mol. Sci. 2021, 22, 11256. https://0-doi-org.brum.beds.ac.uk/10.3390/ijms222011256

AMA Style

Maslivetc V, Laguera B, Chandra S, Dasari R, Olivier WJ, Smith JA, Bissember AC, Masi M, Evidente A, Mathieu V, Kornienko A. Polygodial and Ophiobolin A Analogues for Covalent Crosslinking of Anticancer Targets. International Journal of Molecular Sciences. 2021; 22(20):11256. https://0-doi-org.brum.beds.ac.uk/10.3390/ijms222011256

Chicago/Turabian Style

Maslivetc, Vladimir, Breana Laguera, Sunena Chandra, Ramesh Dasari, Wesley J. Olivier, Jason A. Smith, Alex C. Bissember, Marco Masi, Antonio Evidente, Veronique Mathieu, and Alexander Kornienko. 2021. "Polygodial and Ophiobolin A Analogues for Covalent Crosslinking of Anticancer Targets" International Journal of Molecular Sciences 22, no. 20: 11256. https://0-doi-org.brum.beds.ac.uk/10.3390/ijms222011256

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