Design, synthesis, and preclinical characterization of the selective androgen receptor modulator (SARM) RAD140

Chris P. Miller; Maysoun Shomali; C. Richard Lyttle; Louis St L. O'dea; Hillary Herendeen; Kyla Gallacher; Dottie Paquin; Dennis R. Compton; Bishwabhusan Sahoo; Sean A. Kerrigan; Matthew S. Burge; Michael Nickels; Jennifer L. Green; John A. Katzenellenbogen; Alexei Tchesnokov; Gary Hattersley

doi:10.1021/ml1002508

Design, synthesis, and preclinical characterization of the selective androgen receptor modulator (SARM) RAD140

Chris P. Miller
, Maysoun Shomali
, C. Richard Lyttle
, Louis St L. O'dea
, Hillary Herendeen
, Kyla Gallacher
, Dottie Paquin
, Dennis R. Compton
, Bishwabhusan Sahoo
, Sean A. Kerrigan
, Matthew S. Burge
, Michael Nickels
, Jennifer L. Green
, John A. Katzenellenbogen
, Alexei Tchesnokov
, Gary Hattersley

Chemistry

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

Abstract

This report describes the discovery of RAD140, a potent, orally bioavailable, nonsteroidal selective androgen receptor modulator (SARM). The characterization of RAD140 in several preclinical models of anabolic androgen action is also described.

Original language	English (US)
Pages (from-to)	124-129
Number of pages	6
Journal	ACS Medicinal Chemistry Letters
Volume	2
Issue number	2
DOIs	https://doi.org/10.1021/ml1002508
State	Published - Feb 10 2011

Keywords

Androgen
cachexia
Herschberger assay
oxadiazole
primate
SARM

ASJC Scopus subject areas

Biochemistry
Drug Discovery
Organic Chemistry

Online availability

10.1021/ml1002508

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Miller, C. P., Shomali, M., Lyttle, C. R., O'dea, L. S. L., Herendeen, H., Gallacher, K., Paquin, D., Compton, D. R., Sahoo, B., Kerrigan, S. A., Burge, M. S., Nickels, M., Green, J. L., Katzenellenbogen, J. A., Tchesnokov, A., & Hattersley, G. (2011). Design, synthesis, and preclinical characterization of the selective androgen receptor modulator (SARM) RAD140. ACS Medicinal Chemistry Letters, 2(2), 124-129. https://doi.org/10.1021/ml1002508

Miller, CP, Shomali, M, Lyttle, CR, O'dea, LSL, Herendeen, H, Gallacher, K, Paquin, D, Compton, DR, Sahoo, B, Kerrigan, SA, Burge, MS, Nickels, M, Green, JL, Katzenellenbogen, JA, Tchesnokov, A & Hattersley, G 2011, 'Design, synthesis, and preclinical characterization of the selective androgen receptor modulator (SARM) RAD140', ACS Medicinal Chemistry Letters, vol. 2, no. 2, pp. 124-129. https://doi.org/10.1021/ml1002508

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abstract = "This report describes the discovery of RAD140, a potent, orally bioavailable, nonsteroidal selective androgen receptor modulator (SARM). The characterization of RAD140 in several preclinical models of anabolic androgen action is also described.",

keywords = "Androgen, cachexia, Herschberger assay, oxadiazole, primate, SARM",

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doi = "10.1021/ml1002508",

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AU - Lyttle, C. Richard

AU - O'dea, Louis St L.

AU - Herendeen, Hillary

AU - Gallacher, Kyla

AU - Paquin, Dottie

AU - Compton, Dennis R.

AU - Sahoo, Bishwabhusan

AU - Kerrigan, Sean A.

AU - Burge, Matthew S.

AU - Nickels, Michael

AU - Green, Jennifer L.

AU - Katzenellenbogen, John A.

AU - Tchesnokov, Alexei

AU - Hattersley, Gary

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KW - cachexia

KW - Herschberger assay

KW - oxadiazole

KW - primate

KW - SARM

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Design, synthesis, and preclinical characterization of the selective androgen receptor modulator (SARM) RAD140

Abstract

Keywords

ASJC Scopus subject areas

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