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
Online AccessGet full text

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Abstract [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.
AbstractList 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.
[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.
Author Li, Zhenwu
Neckers, Leonard
Figg, W. Douglas
Beutler, John A.
Sourbier, Carole
Ramos, Joe W.
Hayavi, Sima
Fash, David M.
Sulzmaier, Florian J.
Chain, William J.
Talisman, Ian J.
Peer, Cody J.
AuthorAffiliation d Molecular Targets Laboratory, National Cancer Institute, Frederick, Maryland 21702, United States
e Urologic Oncology Branch, Center for Cancer Research, National Cancer Institute, Frederick, Maryland 21702, United States
b The University of Hawaii Cancer Center, 701 Ilalo Street, Honolulu, Hawaii 96813, United States
a Department of Chemistry, University of Hawaii at Manoa, 2545 McCarthy Mall, Honolulu, Hawaii 96822, United States
c Genitourinary Malignancies Branch, National Cancer Institute, Frederick, Maryland 21702, United States
f Developmental Therapeutics Program, National Cancer Institute, Frederick, Maryland 21702, United States
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Issue 11
Keywords Bioavailability
Englerins
Sesquiterpenes
Cancer
Language English
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Snippet [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...
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...
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SubjectTerms 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
Title Synthesis of a stable and orally bioavailable englerin analogue
URI https://dx.doi.org/10.1016/j.bmcl.2016.04.016
https://www.ncbi.nlm.nih.gov/pubmed/27107948
https://www.proquest.com/docview/1808668178
https://pubmed.ncbi.nlm.nih.gov/PMC4862412
Volume 26
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