Isoxazole-containing 5′ mRNA cap analogues as inhibitors of the translation initiation process

Bioorganic Chemistry, 96, 103583, 2020

Authors: Piecyk Karolina, Lukaszewicz Maciej, Kamel Karol, Janowska Maria, Pietrow Paulina, Kmiecik Sebastian, Jankowska-Anyszka Marzena

Abstract

Herein we describe a synthesis of new isoxazole-containing 5′ mRNA cap analogues via a cycloaddition reaction. The obtained analogues show a capability to inhibit cap-dependent translation in vitro and are characterized by a new binding mode in which an isoxazolic ring, instead of guanine, is involved in the stacking effect. Our study provides valuable information toward designing new compounds that can be potentially used as anticancer therapeutics.

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