Synthesis of guggulsterone derivatives as potential anti-austerity agents against PANC-1 human pancreatic cancer cells.


Journal

Bioorganic & medicinal chemistry letters
ISSN: 1464-3405
Titre abrégé: Bioorg Med Chem Lett
Pays: England
ID NLM: 9107377

Informations de publication

Date de publication:
01 04 2020
Historique:
received: 02 12 2019
revised: 08 01 2020
accepted: 09 01 2020
pubmed: 15 2 2020
medline: 1 4 2021
entrez: 15 2 2020
Statut: ppublish

Résumé

E- and Z-guggulsterones and nine guggulsterone derivatives (GSDs) were synthesized and evaluated for their preferential cytotoxicity against human PANC-1 cell in nutrient deprived medium utilizing antiausterity strategy. Among the synthesized compounds, GSD-1 and GSD-7 showed potent cytotoxicity against PANC-1 cells under nutrient-deprived conditions in a concentration dependent manner, with a PC

Identifiants

pubmed: 32057581
pii: S0960-894X(20)30017-2
doi: 10.1016/j.bmcl.2020.126964
pii:
doi:

Substances chimiques

Antineoplastic Agents 0
Pregnenediones 0
pregna-4,17-diene-3,16-dione A4PW148END

Types de publication

Journal Article Research Support, Non-U.S. Gov't

Langues

eng

Sous-ensembles de citation

IM

Pagination

126964

Informations de copyright

Copyright © 2020 Elsevier Ltd. All rights reserved.

Déclaration de conflit d'intérêts

Declaration of Competing Interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.

Auteurs

Aki Kohyama (A)

Faculty of Pharmaceutical Sciences, University of Toyama, 2630 Sugitani, Toyama 930-0194, Japan.

Rei Yokoyama (R)

Faculty of Pharmaceutical Sciences, University of Toyama, 2630 Sugitani, Toyama 930-0194, Japan.

Dya Fita Dibwe (DF)

Division of Natural Drug Discovery, Institute of Natural Medicine, University of Toyama, 2630 Sugitani, Toyama 930-0194, Japan.

Sahar El-Mekkawy (S)

Department of Chemistry of Natural Compounds, National Research Centre, Elbohouth St., Giza, Egypt.

Meselhy R Meselhy (MR)

Department of Pharmacognosy, Faculty of Pharmacy, Cairo University, Cairo, Egypt.

Suresh Awale (S)

Division of Natural Drug Discovery, Institute of Natural Medicine, University of Toyama, 2630 Sugitani, Toyama 930-0194, Japan. Electronic address: suresh@inm.u-toyama.ac.jp.

Yuji Matsuya (Y)

Faculty of Pharmaceutical Sciences, University of Toyama, 2630 Sugitani, Toyama 930-0194, Japan. Electronic address: matsuya@pha.u-toyama.ac.jp.

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Classifications MeSH