Mono- and bis-pyrazolophthalazines: Design, synthesis, cytotoxic activity, DNA/HSA binding and molecular docking studies.
Animals
Antineoplastic Agents
/ chemical synthesis
Binding Sites
/ drug effects
Cattle
Cell Proliferation
/ drug effects
Cell Survival
/ drug effects
Cells, Cultured
DNA
/ chemistry
Dose-Response Relationship, Drug
Drug Design
Drug Screening Assays, Antitumor
Humans
Molecular Docking Simulation
Molecular Structure
Phthalazines
/ chemical synthesis
Serum Albumin, Human
/ chemistry
Structure-Activity Relationship
Anticancer
Cytotoxic
Human serum albumins (HSA)
Pyrazolophthalazines
Transport proteins
Journal
Bioorganic & medicinal chemistry
ISSN: 1464-3391
Titre abrégé: Bioorg Med Chem
Pays: England
ID NLM: 9413298
Informations de publication
Date de publication:
15 01 2021
15 01 2021
Historique:
received:
11
10
2020
revised:
03
12
2020
accepted:
07
12
2020
pubmed:
23
12
2020
medline:
31
7
2021
entrez:
22
12
2020
Statut:
ppublish
Résumé
In an attempt to find new potent cytotoxic compounds, several mono- and bis-pyrazolophthalazines 4a-m and 6a-h were synthesized through an efficient, one-pot, three- and pseudo five-component synthetic approach. All derivatives were evaluated for their in vitro cytotoxic activities against four human cancer cell lines of A549, HepG2, MCF-7, and HT29. Compound 4e showed low toxicity against normal cell lines (MRC-5 and MCF 10A, IC
Identifiants
pubmed: 33352388
pii: S0968-0896(20)30774-4
doi: 10.1016/j.bmc.2020.115944
pii:
doi:
Substances chimiques
Antineoplastic Agents
0
Phthalazines
0
DNA
9007-49-2
calf thymus DNA
91080-16-9
Serum Albumin, Human
ZIF514RVZR
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
115944Informations de copyright
Copyright © 2020. Published by Elsevier Ltd.