Synthesis of a stable and orally bioavailable englerin analogue

[Display omitted] 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.

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Bibliographic Details
Published inBioorganic & medicinal chemistry letters Vol. 26; no. 11; pp. 2641 - 2644
Main Authors Fash, David M., Peer, Cody J., Li, Zhenwu, Talisman, Ian J., Hayavi, Sima, Sulzmaier, Florian J., Ramos, Joe W., Sourbier, Carole, Neckers, Leonard, Figg, W. Douglas, Beutler, John A., Chain, William J.
Format Journal Article
LanguageEnglish
Published England Elsevier Ltd 01.06.2016
Subjects
Administration, Oral
Animals
Antineoplastic Agents - administration & dosage
Antineoplastic Agents - chemistry
Antineoplastic Agents - pharmacology
Bioavailability
Biological Availability
Cancer
Cell Line, Tumor
Cell Proliferation - drug effects
Dose-Response Relationship, Drug
Drug Screening Assays, Antitumor
Englerins
Humans
Mice
Molecular Structure
Rats
Sesquiterpenes
Sesquiterpenes, Guaiane - administration & dosage
Sesquiterpenes, Guaiane - chemistry
Sesquiterpenes, Guaiane - pharmacology
Structure-Activity Relationship
Bioavailability
Englerins
Sesquiterpenes
Cancer
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Summary:[Display omitted] 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.
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Present address: Department of Chemistry and Biochemistry, University of Delaware, 163 The Green, Newark, Delaware 19716.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2016.04.016