Synthesis and structure-activity studies of the V-ATPase inhibitor saliphenylhalamide (SaliPhe) and simplified analogs

被引：7
|
作者：
Garcia-Rodriguez, Jose [1 ]
Mendiratta, Saurabh [2 ]
White, Michael A. [2 ]
Xie, Xiao-Song [3 ]
De Brabander, Jef K. [1 ]
机构：
[1] Univ Texas SW Med Ctr Dallas, Dept Biochem, Dallas, TX 75390 USA
[2] Univ Texas SW Med Ctr Dallas, Dept Cell Biol, Dallas, TX 75390 USA
[3] Univ Texas SW Med Ctr Dallas, Eugene McDermott Ctr Human Growth & Dev, Dallas, TX 75390 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2015年 / 25卷 / 20期
关键词：
V-ATPase; Antiviral; Anticancer; Benzolactone; Salicylihalamide; FORMAL TOTAL-SYNTHESIS; VACUOLAR H+-ATPASE; SALICYLIHALAMIDE-A; POTENT SALICYLIHALAMIDE; 1,3-DIOL ACETONIDES; CANCER; (-)-SALICYLIHALAMIDE-A; IDENTIFICATION; MECHANISM; INFECTION;
D O I：
10.1016/j.bmcl.2015.09.021
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
An efficient total synthesis of the potent V-ATPase inhibitor saliphenylhalamide (SaliPhe), a synthetic variant of the natural product salicylihalamide A (SaliA), has been accomplished aimed at facilitating the development of SaliPhe as an anticancer and antiviral agent. This new approach enabled facile access to derivatives for structure-activity relationship studies, leading to simplified analogs that maintain SaliPhe's biological properties. These studies will provide a solid foundation for the continued evaluation of SaliPhe and analogs as potential anticancer and antiviral agents. (C) 2015 Elsevier Ltd. All rights reserved.
引用
收藏
页码：4393 / 4398
页数：6
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