Upregulation of p53 through induction of MDM2 degradation: Anthraquinone analogs.

In this study, we systematically investigated the effect of substitution patterns of the core anthraquinone scaffold. Through cytotoxicity evaluation in two leukemia cell lines, the structure-activity relationship of thirty-two analogs has been examined. Several analogs with comparable or improved potency over BW-AQ-101 have been identified. Western-blot assays verified the effect of the potent compounds on the MDM2-p53 axis. The study also suggests new chemical space for further optimization work.
PMID: 31324563 [PubMed - as supplied by publisher]

Source: Bioorganic and Medicinal Chemistry - July 10, 2019 Category: Chemistry Authors: Draganov AB, Yang X, Anifowose A, De La Cruz LKC, Dai C, Ni N, Chen W, De Los Santos Z, Gu L, Zhou M, Wang B Tags: Bioorg Med Chem Source Type: research