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Derivatives of Procaspase-Activating Compound 1 (PAC-1) and Their Anticancer Activities

Derivatives of Procaspase-Activating Compound 1 (PAC-1) and Their Anticancer Activities

Howard S Roth, Paul J Hergenrother

Curr Med Chem. 2016;23(3):201-41.

PMID: 26630918

Abstract:

PAC-1 induces the activation of procaspase-3 in vitro and in cell culture by chelation of inhibitory labile zinc ions via its ortho-hydroxy-N-acylhydrazone moiety. First reported in 2006, PAC-1 has shown promise in cell culture and animal models of cancer, and a Phase I clinical trial in cancer patients began in March 2015 (NCT02355535). Because of the considerable interest in this compound and a well-defined structure-activity relationship, over 1000 PAC-1 derivatives have been synthesized in an effort to vary pharmacological properties such as potency and pharmacokinetics. This article provides a comprehensive examination of all PAC-1 derivatives reported to date. A survey of PAC-1 derivative libraries is provided, with an indepth discussion of four derivatives on which extensive studies have been performed.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP315183212	PAC-1		315183-21-2	Price

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