2. Academic Validation
  3. Synthesis of a stable and orally bioavailable englerin analogue

Synthesis of a stable and orally bioavailable englerin analogue

  • Bioorg Med Chem Lett. 2016 Jun 1;26(11):2641-4. doi: 10.1016/j.bmcl.2016.04.016.
David M Fash 1,  Cody J Peer 2,  Zhenwu Li 1,  Ian J Talisman 1,  Sima Hayavi 3,  Florian J Sulzmaier 4,  Joe W Ramos 4,  Carole Sourbier 5,  Leonard Neckers 5,  W Douglas Figg 2,  John A Beutler 6,  William J Chain 7
Affiliations

Affiliations

  • 1 Department of Chemistry, University of Hawaii at Manoa, 2545 McCarthy Mall, Honolulu, HI 96822, United States.
  • 2 Genitourinary Malignancies Branch, National Cancer Institute, Frederick, MD 21702, United States.
  • 3 Developmental Therapeutics Program, National Cancer Institute, Frederick, MD 21702, United States.
  • 4 The University of Hawaii Cancer Center, 701 Ilalo Street, Honolulu, HI 96813, United States.
  • 5 Urologic Oncology Branch, Center for Cancer Research, National Cancer Institute, Frederick, MD 21702, United States.
  • 6 Molecular Targets Laboratory, National Cancer Institute, Frederick, MD 21702, United States. Electronic address: beutlerj@mail.nih.gov.
  • 7 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.
PMID: 27107948 DOI: 10.1016/j.bmcl.2016.04.016
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.

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