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Polygodial and ophiobolin A analogues for covalent crosslinking of anticancer targets

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posted on 2023-05-21, 03:20 authored by Maslivetc, V, Laguera, B, Chandra, S, Dasari, R, Wesley Olivier, Jason SmithJason Smith, Alexander BissemberAlexander Bissember, Masi, M, Evidente, A, Mathieu, V, Kornienko, A
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.

History

Publication title

International Journal of Molecular Sciences

Volume

22

Issue

20

Article number

11256

Number

11256

Pagination

1-11

ISSN

1422-0067

Department/School

School of Natural Sciences

Publisher

Molecular Diversity Preservation International

Place of publication

Matthaeusstrasse 11, Basel, Switzerland, Ch-4057

Rights 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/).

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  • Open

Socio-economic Objectives

Expanding knowledge in the chemical sciences

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