共 50 条
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
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
相关论文