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Bioorganic & Medicinal Chemistry

Bioorganic & Medicinal Chemistry

IF: 3.3
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Design, synthesis and anti-necroptosis activity of fused heterocyclic MLKL inhibitors

Published:1 March 2024 DOI:
Yining Tang , Chunlin Zhuang

Abstract

Necroptosis is an important form of programmed cell death (PCD), which is mediated by a death receptor and independent of the caspase proteolytic enzyme. Mixed lineage kinase domain-like (MLKL) is the final effector of necroptosis, playing an irreplaceable role in the execution of necroptosis. However, the studies on MLKL inhibitors are in their infancy. Necrosulfonamide (NSA) is an early-discovered covalent MLKL inhibitor, possessing medium anti-necroptosis activity and a structure-activity relationship (SAR) not widely disclosed. In this study, with the covalent motif maintained, we aim to improve the activity by introducing the terminal fused heterocycles and meanwhile revealing the SAR on the part. As a result, compounds 9 and 14 showed the best activity (EC50?=?148.4 and 595.9?nM) against necroptosis among the analogues by covalently binding to MLKL. The SAR was also concluded to guide further structural optimization in this field.

Substances (4)

Materials
Procduct Name CAS Molecular Formula Supplier Price
Z-VAD-FMK 187389-52-2 C22H30FN3O7 316 suppliers $38.00-$5672.00
Z-VAD-FMK 187389-52-2 C22H30FN3O7 316 suppliers $38.00-$5672.00
Z-VAD-FMK 187389-52-2 C22H30FN3O7 316 suppliers $38.00-$5672.00
Z-VAD-FMK 187389-52-2 C22H30FN3O7 316 suppliers $38.00-$5672.00

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