Identification of novel anti-cancer agents by the synthesis and cellular screening of a noscapine-based library.
Anticancer agents
Drug repurposing
Huisgen reaction
Natural product
Noscapine
Papaver
Tubulin-binding
Journal
Bioorganic chemistry
ISSN: 1090-2120
Titre abrégé: Bioorg Chem
Pays: United States
ID NLM: 1303703
Informations de publication
Date de publication:
10 2021
10 2021
Historique:
received:
28
02
2021
revised:
26
06
2021
accepted:
27
06
2021
pubmed:
25
7
2021
medline:
15
12
2021
entrez:
24
7
2021
Statut:
ppublish
Résumé
Noscapine is a natural product first isolated from the opium poppy (Papaver somniferum L.) with anticancer properties. In this work, we report the synthesis and cellular screening of a noscapine-based library. A library of novel noscapine derivatives was synthesized with modifications in the isoquinoline and phthalide scaffolds. The so generated library, consisting of fifty-seven derivatives of the natural product noscapine, was tested against MDA-MB-231 breast cancer cells in a cellular proliferation assay (with a Z' > 0.7). The screening resulted in the identification of two novel noscapine derivatives as inhibitors of MDA cell growth with IC
Identifiants
pubmed: 34303039
pii: S0045-2068(21)00512-5
doi: 10.1016/j.bioorg.2021.105135
pii:
doi:
Substances chimiques
Antineoplastic Agents
0
Benzofurans
0
Isoquinolines
0
Small Molecule Libraries
0
Tubulin
0
Noscapine
8V32U4AOQU
phthalide
8VV922U86J
isoquinoline
JGX76Y85M6
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
105135Informations de copyright
Copyright © 2021 Elsevier Inc. All rights reserved.