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

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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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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

PY - 2011/2/10

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KW - cachexia

KW - Herschberger assay

KW - oxadiazole

KW - primate

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

Abstract

Keywords

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