Polygodial and Ophiobolin A Analogues for Covalent Crosslinking of Anticancer Targets

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dc.contributor.authorMaslivetc, Vladimir
dc.contributor.authorLaguera, Breana
dc.contributor.authorChandra, Sunena
dc.contributor.authorDasari, Ramesh
dc.contributor.authorOlivier, Wesley
dc.contributor.authorSmith, Jason A.
dc.contributor.authorBissember, Alex C.
dc.contributor.authorMasi, Marco
dc.contributor.authorEvidente, Antonio
dc.contributor.authorMathieu, Veronique
dc.contributor.authorKornienko, Alexander
dc.date.accessioned2021-10-19T20:30:53Z
dc.date.available2021-10-19T20:30:53Z
dc.date.issued2021-10-21
dc.description.abstractIn 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.
dc.description.departmentChemistry and Biochemistry
dc.formatText
dc.format.extent11 pages
dc.format.medium1 file (.pdf)
dc.identifier.citationMaslivetc, V., Laguera, B., Chandra, S., Dasari, R., Olivier, W. J., Smith, J. A., Bissember, A. C., Masi, M., Evidente, A., Mathieu, V., & Kornienko, A. (2021). Polygodial and Ophiobolin A analogues for covalent crosslinking of anticancer targets. International Journal of Molecular Sciences, 22(20), 11256.
dc.identifier.doihttps://doi.org/10.3390/ijms222011256
dc.identifier.issn1422-0067
dc.identifier.issn1422-0067
dc.identifier.urihttps://hdl.handle.net/10877/14672
dc.language.isoen
dc.publisherMultidisciplinary Digital Publishing Institute
dc.rights.licenseThis work is licensed under a Creative Commons Attribution 4.0 International License.
dc.sourceInternational Journal of Molecular Sciences, 2021, Vol. 22, No. 20, Article 11256.
dc.subjectanticancer activity
dc.subjectapoptosis resistance
dc.subjectophiobolin A
dc.subjectpolygodial
dc.subjectwittig reaction
dc.subjectChemistry and Biochemistry
dc.titlePolygodial and Ophiobolin A Analogues for Covalent Crosslinking of Anticancer Targets
dc.typeArticle

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