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Ultrasound promoted green synthesis, anticancer evaluation, and molecular docking studies of hydrazines: a pilot trial
- Source :
- Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 37, Iss 1, Pp 135-144 (2022), Journal of Enzyme Inhibition and Medicinal Chemistry, article-version (VoR) Version of Record
- Publication Year :
- 2021
- Publisher :
- Informa UK Limited, 2021.
-
Abstract
- We reported herein an efficient, environmentally friendly synthesis of hydrazine carboxamides (6a���l) in a water-glycerol (6:4) solvent system using ultrasonic irradiation. Ultrasonicated reactions were found to be much faster and more productive than conventional synthesis. The prepared compounds (6a���l) were tested against nine panels of 60 cancer cell lines according to the National Cancer Institute (NCI US) protocol. N-(4-Chlorophenyl)-2-(2-oxoindolin-3-ylidene)hydrazine-1-carboxamide (6b) was discovered to be promising anticancer agents with higher sensitivity against CCRF-CEM, HOP-92, UO-31, RMPI-8226, HL-60(TB), and MDA-MB-468 with percent growth inhibitions (%GIs) of 143.44, 33.46, 33.21, 33.09, 29.81, and 29.55 respectively. Compounds (6a���l) tested showed greater anticancer activity than Imatinib, except for compound 6k. Compounds 6b and 6c were found to be lethal on the CCRF-CEM leukaemia cell line, with %GIs of 143.44 and 108.91, respectively. Furthermore, molecular docking analysis was performed to investigate ligand binding affinity at the active site of epidermal growth factor (EGFR).
- Subjects :
- Glycerol
Antineoplastic Agents
water: glycerol system
RM1-950
anticancer
Structure-Activity Relationship
Cell Line, Tumor
hydrazine carboxamide
Drug Discovery
egfr inhibitor
Humans
Cell Proliferation
Pharmacology
Dose-Response Relationship, Drug
Molecular Structure
ultrasound
Water
General Medicine
Molecular Docking Simulation
Hydrazines
Ultrasonic Waves
Drug Design
Therapeutics. Pharmacology
Drug Screening Assays, Antitumor
Research Article
Research Paper
Subjects
Details
- ISSN :
- 14756374 and 14756366
- Volume :
- 37
- Database :
- OpenAIRE
- Journal :
- Journal of Enzyme Inhibition and Medicinal Chemistry
- Accession number :
- edsair.doi.dedup.....6f713cfdcbf850bc70223b6d033df78e
- Full Text :
- https://doi.org/10.1080/14756366.2021.1995727