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

Jose Garcia-Rodriguez; Saurabh Mendiratta; Michael A. White; Xiao Song Xie; Jef K. De Brabander

doi:10.1016/j.bmcl.2015.09.021

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

Jose Garcia-Rodriguez, Saurabh Mendiratta, Michael A. White, Xiao Song Xie, Jef K. De Brabander

Research output: Contribution to journal › Article › peer-review

8 Scopus citations

Abstract

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.

Original language	English (US)
Pages (from-to)	4393-4398
Number of pages	6
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	25
Issue number	20
DOIs	https://doi.org/10.1016/j.bmcl.2015.09.021
State	Published - Oct 15 2015

Keywords

Anticancer
Antiviral
Benzolactone
Salicylihalamide
V-ATPase

ASJC Scopus subject areas

Biochemistry
Molecular Medicine
Molecular Biology
Pharmaceutical Science
Drug Discovery
Clinical Biochemistry
Organic Chemistry

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10.1016/j.bmcl.2015.09.021

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

abstract = "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.",

keywords = "Anticancer, Antiviral, Benzolactone, Salicylihalamide, V-ATPase",

author = "Jose Garcia-Rodriguez and Saurabh Mendiratta and White, {Michael A.} and Xie, {Xiao Song} and {De Brabander}, {Jef K.}",

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AU - Garcia-Rodriguez, Jose

AU - Mendiratta, Saurabh

AU - White, Michael A.

AU - Xie, Xiao Song

AU - De Brabander, Jef K.

PY - 2015/10/15

Y1 - 2015/10/15

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AB - 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.

KW - Anticancer

KW - Antiviral

KW - Benzolactone

KW - Salicylihalamide

KW - V-ATPase

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

Abstract

Keywords

ASJC Scopus subject areas

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