147233 - Polygodial and ophiobolin A analogues for covalent crosslinking of anticancer targets.pdf (1.03 MB)
Download filePolygodial and ophiobolin A analogues for covalent crosslinking of anticancer targets
journal contribution
posted on 2023-05-21, 03:20 authored by Maslivetc, V, Laguera, B, Chandra, S, Dasari, R, Wesley OlivierWesley Olivier, Jason SmithJason Smith, Alexander BissemberAlexander Bissember, Masi, M, Evidente, A, Mathieu, V, Kornienko, AIn 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.
History
Publication title
International Journal of Molecular SciencesVolume
22Issue
20Article number
11256Number
11256Pagination
1-11ISSN
1422-0067Department/School
School of Natural SciencesPublisher
Molecular Diversity Preservation InternationalPlace of publication
Matthaeusstrasse 11, Basel, Switzerland, Ch-4057Rights statement
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 (https://creativecommons.org/licenses/by/4.0/).Repository Status
- Open