Synthesis of a stable and orally bioavailable englerin analogue

David M. Fash; Cody J. Peer; Zhenwu Li; Ian J. Talisman; Sima Hayavi; Florian J. Sulzmaier; Joe W. Ramos; Carole Sourbier; Leonard Neckers; W. Douglas Figg; John A. Beutler; William J. Chain

doi:10.1016/j.bmcl.2016.04.016

Synthesis of a stable and orally bioavailable englerin analogue

David M. Fash, Cody J. Peer, Zhenwu Li, Ian J. Talisman, Sima Hayavi, Florian J. Sulzmaier, Joe W. Ramos, Carole Sourbier, Leonard Neckers, W. Douglas Figg, John A. Beutler^*, William J. Chain

^*Corresponding author for this work

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

10 Scopus citations

Abstract

Synthesis of analogues of englerin A with a reduced propensity for hydrolysis of the glycolate moiety led to a compound which possessed the renal cancer cell selectivity of the parent and was orally bioavailable in mice.

Original language	English
Pages (from-to)	2641-2644
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	26
Issue number	11
DOIs	https://doi.org/10.1016/j.bmcl.2016.04.016
State	Published - 1 Jun 2016
Externally published	Yes

Keywords

Bioavailability
Cancer
Englerins
Sesquiterpenes

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title = "Synthesis of a stable and orally bioavailable englerin analogue",

abstract = "Synthesis of analogues of englerin A with a reduced propensity for hydrolysis of the glycolate moiety led to a compound which possessed the renal cancer cell selectivity of the parent and was orally bioavailable in mice.",

keywords = "Bioavailability, Cancer, Englerins, Sesquiterpenes",

author = "Fash, {David M.} and Peer, {Cody J.} and Zhenwu Li and Talisman, {Ian J.} and Sima Hayavi and Sulzmaier, {Florian J.} and Ramos, {Joe W.} and Carole Sourbier and Leonard Neckers and Figg, {W. Douglas} and Beutler, {John A.} and Chain, {William J.}",

year = "2016",

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doi = "10.1016/j.bmcl.2016.04.016",

language = "English",

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journal = "Bioorganic and Medicinal Chemistry Letters",

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TY - JOUR

T1 - Synthesis of a stable and orally bioavailable englerin analogue

AU - Fash, David M.

AU - Peer, Cody J.

AU - Li, Zhenwu

AU - Talisman, Ian J.

AU - Hayavi, Sima

AU - Sulzmaier, Florian J.

AU - Ramos, Joe W.

AU - Sourbier, Carole

AU - Neckers, Leonard

AU - Figg, W. Douglas

AU - Beutler, John A.

AU - Chain, William J.

PY - 2016/6/1

Y1 - 2016/6/1

N2 - Synthesis of analogues of englerin A with a reduced propensity for hydrolysis of the glycolate moiety led to a compound which possessed the renal cancer cell selectivity of the parent and was orally bioavailable in mice.

AB - Synthesis of analogues of englerin A with a reduced propensity for hydrolysis of the glycolate moiety led to a compound which possessed the renal cancer cell selectivity of the parent and was orally bioavailable in mice.

KW - Bioavailability

KW - Cancer

KW - Englerins

KW - Sesquiterpenes

UR - http://www.scopus.com/inward/record.url?scp=84963964103&partnerID=8YFLogxK

U2 - 10.1016/j.bmcl.2016.04.016

DO - 10.1016/j.bmcl.2016.04.016

M3 - Article

C2 - 27107948

AN - SCOPUS:84963964103

SN - 0960-894X

VL - 26

SP - 2641

EP - 2644

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 11

ER -

Synthesis of a stable and orally bioavailable englerin analogue

Abstract

Keywords

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