Discovery of a synthetic dual inhibitor of HIV and HCV infection based on a tetrabutoxy-calix[4]arene scaffold

Lun K. Tsou; Ginger E. Dutschman; Elizabeth A. Gullen; Maria Telpoukhovskaia; Yung Chi Cheng; Andrew D. Hamilton

doi:10.1016/j.bmcl.2010.02.043

Discovery of a synthetic dual inhibitor of HIV and HCV infection based on a tetrabutoxy-calix[4]arene scaffold

Lun K. Tsou, Ginger E. Dutschman, Elizabeth A. Gullen, Maria Telpoukhovskaia, Yung Chi Cheng, Andrew D. Hamilton

Chemistry

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

Abstract

A potential anti-HIV and HCV drug candidate is highly desirable as coinfection has become a worldwide public health challenge. A potent compound based on a tetrabutoxy-calix[4]arene scaffold that possesses dual inhibition for both HIV and HCV is described. Structural activity relationship studies demonstrate the effects of lower-rim alkylation in maintaining cone conformation and upper-rim interacting head groups on the calix[4]arene play key roles for its potent dual antiviral activities.

Original language	English (US)
Pages (from-to)	2137-2139
Number of pages	3
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	20
Issue number	7
DOIs	https://doi.org/10.1016/j.bmcl.2010.02.043
State	Published - Apr 1 2010

Keywords

Calixarenes
HIV-HCV coinfection inhibitors
Protein surface recognition

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.2010.02.043

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title = "Discovery of a synthetic dual inhibitor of HIV and HCV infection based on a tetrabutoxy-calix[4]arene scaffold",

abstract = "A potential anti-HIV and HCV drug candidate is highly desirable as coinfection has become a worldwide public health challenge. A potent compound based on a tetrabutoxy-calix[4]arene scaffold that possesses dual inhibition for both HIV and HCV is described. Structural activity relationship studies demonstrate the effects of lower-rim alkylation in maintaining cone conformation and upper-rim interacting head groups on the calix[4]arene play key roles for its potent dual antiviral activities.",

keywords = "Calixarenes, HIV-HCV coinfection inhibitors, Protein surface recognition",

author = "Tsou, {Lun K.} and Dutschman, {Ginger E.} and Gullen, {Elizabeth A.} and Maria Telpoukhovskaia and Cheng, {Yung Chi} and Hamilton, {Andrew D.}",

note = "Funding Information: We thank the National Institutes of Health ( GM 35208 to A.D.H) and ( AI 38204 to Y.-C.C.) for financial support of this work.",

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doi = "10.1016/j.bmcl.2010.02.043",

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T1 - Discovery of a synthetic dual inhibitor of HIV and HCV infection based on a tetrabutoxy-calix[4]arene scaffold

AU - Tsou, Lun K.

AU - Dutschman, Ginger E.

AU - Gullen, Elizabeth A.

AU - Telpoukhovskaia, Maria

AU - Cheng, Yung Chi

AU - Hamilton, Andrew D.

N1 - Funding Information: We thank the National Institutes of Health ( GM 35208 to A.D.H) and ( AI 38204 to Y.-C.C.) for financial support of this work.

PY - 2010/4/1

Y1 - 2010/4/1

N2 - A potential anti-HIV and HCV drug candidate is highly desirable as coinfection has become a worldwide public health challenge. A potent compound based on a tetrabutoxy-calix[4]arene scaffold that possesses dual inhibition for both HIV and HCV is described. Structural activity relationship studies demonstrate the effects of lower-rim alkylation in maintaining cone conformation and upper-rim interacting head groups on the calix[4]arene play key roles for its potent dual antiviral activities.

AB - A potential anti-HIV and HCV drug candidate is highly desirable as coinfection has become a worldwide public health challenge. A potent compound based on a tetrabutoxy-calix[4]arene scaffold that possesses dual inhibition for both HIV and HCV is described. Structural activity relationship studies demonstrate the effects of lower-rim alkylation in maintaining cone conformation and upper-rim interacting head groups on the calix[4]arene play key roles for its potent dual antiviral activities.

KW - Calixarenes

KW - HIV-HCV coinfection inhibitors

KW - Protein surface recognition

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Discovery of a synthetic dual inhibitor of HIV and HCV infection based on a tetrabutoxy-calix[4]arene scaffold

Abstract

Keywords

ASJC Scopus subject areas

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