Synthesis of a stable and orally bioavailable englerin analogue.
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.
Department of Chemistry, University of Hawaii at Manoa, 2545 McCarthy Mall, Honolulu, HI 96822, United States.
David M
DM
Fash
Genitourinary Malignancies Branch, National Cancer Institute, Frederick, MD 21702, United States.
Cody J
CJ
Peer
Department of Chemistry, University of Hawaii at Manoa, 2545 McCarthy Mall, Honolulu, HI 96822, United States.
Zhenwu
Z
Li
Department of Chemistry, University of Hawaii at Manoa, 2545 McCarthy Mall, Honolulu, HI 96822, United States.
Ian J
IJ
Talisman
Developmental Therapeutics Program, National Cancer Institute, Frederick, MD 21702, United States.
Sima
S
Hayavi
The University of Hawaii Cancer Center, 701 Ilalo Street, Honolulu, HI 96813, United States.
Florian J
FJ
Sulzmaier
The University of Hawaii Cancer Center, 701 Ilalo Street, Honolulu, HI 96813, United States.
Joe W
JW
Ramos
Urologic Oncology Branch, Center for Cancer Research, National Cancer Institute, Frederick, MD 21702, United States.
Carole
C
Sourbier
Urologic Oncology Branch, Center for Cancer Research, National Cancer Institute, Frederick, MD 21702, United States.
Leonard
L
Neckers
Genitourinary Malignancies Branch, National Cancer Institute, Frederick, MD 21702, United States.
W Douglas
WD
Figg
Molecular Targets Laboratory, National Cancer Institute, Frederick, MD 21702, United States. Electronic address: beutlerj@mail.nih.gov.
John A
JA
Beutler
Department of Chemistry, University of Hawaii at Manoa, 2545 McCarthy Mall, Honolulu, HI 96822, United States; The University of Hawaii Cancer Center, 701 Ilalo Street, Honolulu, HI 96813, United States. Electronic address: wchain@udel.edu.
William J
WJ
Chain
D000284:Administration, Oral; D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology*; D001682:Biological Availability; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D051379:Mice; D015394:Molecular Structure; D051381:Rats; D045789:Sesquiterpenes, Guaiane / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D000970:Antineoplastic Agents; D045789:Sesquiterpenes, Guaiane; C534971:englerin A
Bioavailability; Cancer; Englerins; Sesquiterpenes