Design, synthesis, and biological activity of bicyclic radester analogues as Hsp90 inhibitors

Vinod D. Jadhav; Adam S. Duerfeldt; Brian S.J. Blagg

doi:10.1016/j.bmcl.2009.10.091

Design, synthesis, and biological activity of bicyclic radester analogues as Hsp90 inhibitors

Vinod D. Jadhav, Adam S. Duerfeldt, Brian S.J. Blagg

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

9 Scopus citations

Abstract

Bicyclic radester analogues have been synthesized and evaluated for Hsp90 inhibitory activity. These analogues induce concentration-dependent degradation of Hsp90-dependent client proteins with the six-membered bicyclic analogues manifesting increased activity versus the five-membered counterparts.

Original language	English (US)
Pages (from-to)	6845-6850
Number of pages	6
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	19
Issue number	24
DOIs	https://doi.org/10.1016/j.bmcl.2009.10.091
State	Published - Dec 15 2009
Externally published	Yes

Bibliographical note

Funding Information:
The authors gratefully acknowledge NIH/NCI CA 109265, the Madison and Lila Self Graduate Fellowship (A.S.D.) and the American Foundation of Pharmaceutical Education for financial support (A.S.D.).

Keywords

Anti-cancer
Geldanamycin
Hsp90
Radicicol

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

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10.1016/j.bmcl.2009.10.091

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title = "Design, synthesis, and biological activity of bicyclic radester analogues as Hsp90 inhibitors",

abstract = "Bicyclic radester analogues have been synthesized and evaluated for Hsp90 inhibitory activity. These analogues induce concentration-dependent degradation of Hsp90-dependent client proteins with the six-membered bicyclic analogues manifesting increased activity versus the five-membered counterparts.",

keywords = "Anti-cancer, Geldanamycin, Hsp90, Radicicol",

author = "Jadhav, {Vinod D.} and Duerfeldt, {Adam S.} and Blagg, {Brian S.J.}",

note = "Funding Information: The authors gratefully acknowledge NIH/NCI CA 109265, the Madison and Lila Self Graduate Fellowship (A.S.D.) and the American Foundation of Pharmaceutical Education for financial support (A.S.D.).",

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AU - Jadhav, Vinod D.

AU - Duerfeldt, Adam S.

AU - Blagg, Brian S.J.

N1 - Funding Information: The authors gratefully acknowledge NIH/NCI CA 109265, the Madison and Lila Self Graduate Fellowship (A.S.D.) and the American Foundation of Pharmaceutical Education for financial support (A.S.D.).

PY - 2009/12/15

Y1 - 2009/12/15

N2 - Bicyclic radester analogues have been synthesized and evaluated for Hsp90 inhibitory activity. These analogues induce concentration-dependent degradation of Hsp90-dependent client proteins with the six-membered bicyclic analogues manifesting increased activity versus the five-membered counterparts.

AB - Bicyclic radester analogues have been synthesized and evaluated for Hsp90 inhibitory activity. These analogues induce concentration-dependent degradation of Hsp90-dependent client proteins with the six-membered bicyclic analogues manifesting increased activity versus the five-membered counterparts.

KW - Anti-cancer

KW - Geldanamycin

KW - Hsp90

KW - Radicicol

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JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

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ER -

Design, synthesis, and biological activity of bicyclic radester analogues as Hsp90 inhibitors

Abstract

Bibliographical note

Keywords

UN SDGs

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