HIF-1α inhibition by MO-2097, a novel chiral-free benzofuran targeting hnRNPA2B1.

ABSTRACT:

Introduction

Hypoxia-inducible factor 1 (HIF-1) is a transcriptional activator mediating adaptive responses to hypoxia. It is up-regulated in the tumor microenvironment and recognized as an effective anticancer drug target. Previously, we discovered that the natural compound moracin-O and its synthetic derivative MO-460 inhibited HIF-1α via hnRNPA2B1.

Objectives

This study aimed to develop novel HIF-1 inhibitors for cancer chemotherapy by harnessing the potential of the natural products moracins-O and P.

Methods

In an ongoing search for novel HIF-1 inhibitors, a series of nature-inspired benzofurans with modifications on the chiral rings of moracins-O and P were synthesized. They showed improved chemical tractability and were evaluated for their inhibitory activity on

SUBMITTER: Han HJ 

PROVIDER: S-EPMC11464424 | biostudies-literature | 2024 Oct

REPOSITORIES: biostudies-literature