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

Access to Document

10.1016/j.bmcl.2016.04.016

Cite this

@article{2d0ef898e4f34390bde8c120f99c356b,

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",

month = jun,

day = "1",

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

language = "English",

volume = "26",

pages = "2641--2644",

journal = "Bioorganic and Medicinal Chemistry Letters",

issn = "0960-894X",

publisher = "Elsevier Ltd",

number = "11",

}

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 - https://www.scopus.com/pages/publications/84963964103

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

Access to Document

Fingerprint

Cite this