Novel urea linked ciprofloxacin-chalcone hybrids having antiproliferative topoisomerases I/II inhibitory activities and caspases-mediated apoptosis.
Antineoplastic Agents
/ chemical synthesis
Apoptosis
/ drug effects
Caspases
/ metabolism
Catalytic Domain
Cell Line, Tumor
Chalcones
/ chemical synthesis
Ciprofloxacin
/ analogs & derivatives
DNA Topoisomerases, Type I
/ chemistry
DNA Topoisomerases, Type II
/ chemistry
Drug Screening Assays, Antitumor
G2 Phase Cell Cycle Checkpoints
/ drug effects
Humans
Molecular Docking Simulation
Molecular Structure
Phenylurea Compounds
/ chemical synthesis
Poly-ADP-Ribose Binding Proteins
/ chemistry
Protein Binding
Proto-Oncogene Proteins c-bcl-2
/ metabolism
Structure-Activity Relationship
Topoisomerase Inhibitors
/ chemical synthesis
bcl-2-Associated X Protein
/ metabolism
Antiproliferative
Apoptosis
Ciprofloxacin
Molecular docking
Topoisomerases
Journal
Bioorganic chemistry
ISSN: 1090-2120
Titre abrégé: Bioorg Chem
Pays: United States
ID NLM: 1303703
Informations de publication
Date de publication:
01 2021
01 2021
Historique:
received:
23
06
2020
revised:
17
10
2020
accepted:
20
10
2020
pubmed:
30
11
2020
medline:
4
9
2021
entrez:
29
11
2020
Statut:
ppublish
Résumé
A novel series of urea-linked ciprofloxacin (CP)-chalcone hybrids 3a-j were synthesized and screened by NCI-60 cancer cell lines as potential cytotoxic agents. Interestingly, compounds 3c and 3j showed remarkable antiproliferative activities against both colon HCT-116 and leukemia SR cancer cells compared to camptothecin, topotecan and staurosporine with IC
Identifiants
pubmed: 33248713
pii: S0045-2068(20)31720-X
doi: 10.1016/j.bioorg.2020.104422
pii:
doi:
Substances chimiques
Antineoplastic Agents
0
BAX protein, human
0
BCL2 protein, human
0
Chalcones
0
Phenylurea Compounds
0
Poly-ADP-Ribose Binding Proteins
0
Proto-Oncogene Proteins c-bcl-2
0
Topoisomerase Inhibitors
0
bcl-2-Associated X Protein
0
Ciprofloxacin
5E8K9I0O4U
Caspases
EC 3.4.22.-
DNA Topoisomerases, Type I
EC 5.99.1.2
TOP1 protein, human
EC 5.99.1.2
DNA Topoisomerases, Type II
EC 5.99.1.3
TOP2B protein, human
EC 5.99.1.3
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
104422Informations de copyright
Copyright © 2020. Published by Elsevier Inc.