New chalcone-sulfonamide hybrids exhibiting anticancer and antituberculosis activity.
3T3 Cells
Animals
Antineoplastic Agents
/ chemical synthesis
Antitubercular Agents
/ chemical synthesis
Cell Line, Tumor
Chalcones
/ chemical synthesis
Drug Screening Assays, Antitumor
Humans
Mice
Microbial Sensitivity Tests
Molecular Structure
Mycobacterium tuberculosis
/ drug effects
Sulfonamides
/ chemical synthesis
Antibacterial
Anticancer
Antituberculosis
Chalcones
Sulfonamides
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:
15 Aug 2019
15 Aug 2019
Historique:
received:
27
11
2018
revised:
07
02
2019
accepted:
06
05
2019
pubmed:
17
5
2019
medline:
23
7
2019
entrez:
17
5
2019
Statut:
ppublish
Résumé
New sulfonamides 5/6 derived from 4-methoxyacetophenone 1 were synthesized by N-sulfonation reaction of ammonia (3) and aminopyrimidinone (4) with its sulfonyl chloride derivative 2. Sulfonamides 5 and 6 were used as precursors of two new series of chalcones 8a-f and 9a-f, which were obtained through Claisen-Schmidt condensation with aromatic aldehydes 7a-f. Compounds 5/6, 8a-d, 8f, 9a-d, and 9f were screened by the US National Cancer Institute (NCI) at 10 μM against sixty different human cancer cell lines (one-dose trial). Chalcones 8b and 9b satisfied the pre-determined threshold inhibition criteria and were selected for screening at five different concentrations (100, 10, 1.0, 0.1, and 0.01 μM). Compound 8b exhibited remarkable GI
Identifiants
pubmed: 31096118
pii: S0223-5234(19)30422-2
doi: 10.1016/j.ejmech.2019.05.013
pii:
doi:
Substances chimiques
Antineoplastic Agents
0
Antitubercular Agents
0
Chalcones
0
Sulfonamides
0
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
50-60Informations de copyright
Copyright © 2019 Elsevier Masson SAS. All rights reserved.