Small molecule biaryl FSH receptor agonists. Part 1: Lead discovery via encoded combinatorial synthesis

Tao Guo; Anton E.P. Adang; Roland E. Dolle; Guizhen Dong; Dan Fitzpatrick; Peng Geng; Koc Kan Ho; Steven G. Kultgen; Ruiyan Liu; Edward McDonald; Brian F. McGuinness; Kurt W. Saionz; Kenneth J. Valenzano; Nicole C.R. Van Straten; Dan Xie; Maria L. Webb

doi:10.1016/j.bmcl.2004.01.042

Small molecule biaryl FSH receptor agonists. Part 1: Lead discovery via encoded combinatorial synthesis

Tao Guo, Anton E.P. Adang, Roland E. Dolle, Guizhen Dong, Dan Fitzpatrick, Peng Geng, Koc Kan Ho, Steven G. Kultgen, Ruiyan Liu, Edward McDonald, Brian F. McGuinness, Kurt W. Saionz, Kenneth J. Valenzano, Nicole C.R. Van Straten, Dan Xie, Maria L. Webb

Research output: Contribution to journal › Article

41 Scopus citations

Abstract

High-throughput screening of two million compounds in 37 distinct encoded combinatorial libraries using FSH receptor transfected cells provided small molecule agonists such as 1 (EC₅₀=3 μM) and 2 (EC₅₀=3. 9 μM), based on which a focused combinatorial library with a total of 31,372 compounds was designed, synthesized, and screened to reveal 72 novel biaryl FSH receptor agonists such as 8a-c as well as a unique combinatorial SAR.

Original language	English
Pages (from-to)	1713-1716
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	14
Issue number	7
DOIs	https://doi.org/10.1016/j.bmcl.2004.01.042
State	Published - Apr 1 2004
Externally published	Yes

Keywords

Combinatorial synthesis
Small molecule biaryl FSH agonists

Access to Document

10.1016/j.bmcl.2004.01.042

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Guo, T., Adang, A. E. P., Dolle, R. E., Dong, G., Fitzpatrick, D., Geng, P., Ho, K. K., Kultgen, S. G., Liu, R., McDonald, E., McGuinness, B. F., Saionz, K. W., Valenzano, K. J., Van Straten, N. C. R., Xie, D., & Webb, M. L. (2004). Small molecule biaryl FSH receptor agonists. Part 1: Lead discovery via encoded combinatorial synthesis. Bioorganic and Medicinal Chemistry Letters, 14(7), 1713-1716. https://doi.org/10.1016/j.bmcl.2004.01.042

Guo, Tao ; Adang, Anton E.P. ; Dolle, Roland E. ; Dong, Guizhen ; Fitzpatrick, Dan ; Geng, Peng ; Ho, Koc Kan ; Kultgen, Steven G. ; Liu, Ruiyan ; McDonald, Edward ; McGuinness, Brian F. ; Saionz, Kurt W. ; Valenzano, Kenneth J. ; Van Straten, Nicole C.R. ; Xie, Dan ; Webb, Maria L. / Small molecule biaryl FSH receptor agonists. Part 1 : Lead discovery via encoded combinatorial synthesis. In: Bioorganic and Medicinal Chemistry Letters. 2004 ; Vol. 14, No. 7. pp. 1713-1716.

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title = "Small molecule biaryl FSH receptor agonists. Part 1: Lead discovery via encoded combinatorial synthesis",

abstract = "High-throughput screening of two million compounds in 37 distinct encoded combinatorial libraries using FSH receptor transfected cells provided small molecule agonists such as 1 (EC50=3 μM) and 2 (EC50=3. 9 μM), based on which a focused combinatorial library with a total of 31,372 compounds was designed, synthesized, and screened to reveal 72 novel biaryl FSH receptor agonists such as 8a-c as well as a unique combinatorial SAR.",

keywords = "Combinatorial synthesis, Small molecule biaryl FSH agonists",

author = "Tao Guo and Adang, {Anton E.P.} and Dolle, {Roland E.} and Guizhen Dong and Dan Fitzpatrick and Peng Geng and Ho, {Koc Kan} and Kultgen, {Steven G.} and Ruiyan Liu and Edward McDonald and McGuinness, {Brian F.} and Saionz, {Kurt W.} and Valenzano, {Kenneth J.} and {Van Straten}, {Nicole C.R.} and Dan Xie and Webb, {Maria L.}",

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doi = "10.1016/j.bmcl.2004.01.042",

language = "English",

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Guo, T, Adang, AEP, Dolle, RE, Dong, G, Fitzpatrick, D, Geng, P, Ho, KK, Kultgen, SG, Liu, R, McDonald, E, McGuinness, BF, Saionz, KW, Valenzano, KJ, Van Straten, NCR, Xie, D & Webb, ML 2004, 'Small molecule biaryl FSH receptor agonists. Part 1: Lead discovery via encoded combinatorial synthesis', Bioorganic and Medicinal Chemistry Letters, vol. 14, no. 7, pp. 1713-1716. https://doi.org/10.1016/j.bmcl.2004.01.042

Small molecule biaryl FSH receptor agonists. Part 1 : Lead discovery via encoded combinatorial synthesis. / Guo, Tao; Adang, Anton E.P.; Dolle, Roland E.; Dong, Guizhen; Fitzpatrick, Dan; Geng, Peng; Ho, Koc Kan; Kultgen, Steven G.; Liu, Ruiyan; McDonald, Edward; McGuinness, Brian F.; Saionz, Kurt W.; Valenzano, Kenneth J.; Van Straten, Nicole C.R.; Xie, Dan; Webb, Maria L.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 14, No. 7, 01.04.2004, p. 1713-1716.

Research output: Contribution to journal › Article

TY - JOUR

T1 - Small molecule biaryl FSH receptor agonists. Part 1

T2 - Lead discovery via encoded combinatorial synthesis

AU - Guo, Tao

AU - Adang, Anton E.P.

AU - Dolle, Roland E.

AU - Dong, Guizhen

AU - Fitzpatrick, Dan

AU - Geng, Peng

AU - Ho, Koc Kan

AU - Kultgen, Steven G.

AU - Liu, Ruiyan

AU - McDonald, Edward

AU - McGuinness, Brian F.

AU - Saionz, Kurt W.

AU - Valenzano, Kenneth J.

AU - Van Straten, Nicole C.R.

AU - Xie, Dan

AU - Webb, Maria L.

PY - 2004/4/1

Y1 - 2004/4/1

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KW - Combinatorial synthesis

KW - Small molecule biaryl FSH agonists

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