Biological screening of cucurbitacin inspired estrone analogs targeting mitogen-activated protein kinase (MAPK) pathway

Mahmoud S. Ahmed, Fardous El-Senduny, Jessica Taylor, Fathi T. Halaweish

Research output: Contribution to journalArticle

6 Scopus citations

Abstract

Assembly of cucurbitacin inspired estrone analogs has been previously synthesized and screened against melanoma cell lines. Further synthetic optimization was executed via installation of Azide polar functional moiety across 23, 24 α, β-unsaturated ketone side chain using Michael addition reaction. This was followed by biological screening against melanoma cell lines employing MTT assay, in-cell-based ELISA assay, and Western blot analysis to monitor the potential of the synthesized analogs to inhibit the phosphorylated ERK levels. This resulted in evolution of MH-4 possessing IC50 of 3.59 μm with significant decrease in the p-ERK and targeting MAPK pathway.

Original languageEnglish (US)
JournalChemical Biology and Drug Design
Volume2017
DOIs
StatePublished - Jan 1 2017
Externally publishedYes

Keywords

  • Cucurbitacins
  • Estrone
  • MAPK pathway
  • Melanoma
  • Michael addition

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Pharmacology
  • Drug Discovery
  • Organic Chemistry

Fingerprint Dive into the research topics of 'Biological screening of cucurbitacin inspired estrone analogs targeting mitogen-activated protein kinase (MAPK) pathway'. Together they form a unique fingerprint.

  • Cite this