Cucurbitacins inspired organic synthesis: Potential dual inhibitors targeting EGFR - MAPK pathway.
Antineoplastic Agents
/ chemical synthesis
Cell Movement
/ drug effects
Cell Proliferation
/ drug effects
Cucurbitacins
/ chemical synthesis
Dose-Response Relationship, Drug
Drug Screening Assays, Antitumor
ErbB Receptors
/ antagonists & inhibitors
Hep G2 Cells
Humans
MAP Kinase Signaling System
/ drug effects
Models, Molecular
Molecular Structure
Protein Kinase Inhibitors
/ chemical synthesis
Structure-Activity Relationship
Biological oriented organic synthesis
Cucurbitacins
Diastereomers
EGFR
Estrone
MAPK pathway
Journal
European journal of medicinal chemistry
ISSN: 1768-3254
Titre abrégé: Eur J Med Chem
Pays: France
ID NLM: 0420510
Informations de publication
Date de publication:
01 Jul 2019
01 Jul 2019
Historique:
received:
19
02
2019
revised:
19
03
2019
accepted:
09
04
2019
pubmed:
26
4
2019
medline:
18
6
2019
entrez:
26
4
2019
Statut:
ppublish
Résumé
Natural products have been known as a fundamental source for drug discovery leading to the evolution of Biological Oriented Organic Synthesis (BIOS) approach to assemble natural product mimics. Herein, a series of Cucurbitacin inspired estrone analogs was assembled to generate 18 novel synthesized analogs via installation of double bond across C-16/C-17 positions of estrone scaffold and diastereomeric separation of (R) and (S) at C-20. This was followed by biological screening against HEPG-2 cell lines to exhibit anti-proliferative activity ranging from IC
Identifiants
pubmed: 31022583
pii: S0223-5234(19)30324-1
doi: 10.1016/j.ejmech.2019.04.018
pii:
doi:
Substances chimiques
Antineoplastic Agents
0
Protein Kinase Inhibitors
0
Cucurbitacins
60137-06-6
EGFR protein, human
EC 2.7.10.1
ErbB Receptors
EC 2.7.10.1
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
294-304Informations de copyright
Copyright © 2019 Elsevier Masson SAS. All rights reserved.