Strategies for the design of analogs of auranofin endowed with anticancer potential

作     者：Vitali, Valentina Massai, Lara Messori, Luigi 

作者机构：Univ Florence Dept Chem Ugo Schiff Lab Met Med MetMed Via Lastruccia 3 I-50019 Sesto Fiorentino Italy 

出 版 物：《EXPERT OPINION ON DRUG DISCOVERY》 (药物发明专家评论)

年 卷 期：2024年第19卷第7期

页      面：855-867页

核心收录：

学科分类：1007[医学-药学(可授医学、理学学位)] 10[医学] 

基　　金：Fondazione Italiana per la Ricerca sul Cancro (AIRC) [IG26169] PRIN Project [2022JMFC3X] 

主　　题：Anticancer therapy chemical modification drug design gold drugs structure-function relationships 

摘      要：IntroductionAuranofin (AF) is a well-established, FDA-approved, antiarthritic gold drug that is currently being reevaluated for a variety of therapeutic indications through drug repurposing. AF has shown great promise as a potential anticancer agent and has been approved for a few clinical trials in cancer. The renewed interest in AF has led to extensive research into the design, preparation and biological evaluation of auranofin analogs, which may have an even better pharmacological profile than the parent *** coveredThis article reviews the strategies for chemical modification of the AF scaffold. Several auranofin analogs have been prepared and characterized for medical application in the field of cancer treatment over the last 20 years. Some emerging structure-function relationships are proposed and *** opinionThe chemical modification of the AF scaffold has been the subject of intense activity in recent years and this strategy has led to the preparation and evaluation of several AF analogs. The case of iodauranofin is a particularly promising example. The availability of homogeneous biological data for a group of AF derivatives allows some initial structure-function relationships to be proposed, which may inspire the design and synthesis of new and better AF analogs for cancer treatment.