HOMEPRODUCTSCOMPANYCONTACTFAQResearchDictionaryPharmaSign Up FREE or Login

Synthesis, spectroscopic properties, molecular docking, anti-colon cancer and anti-microbial studies of some novel metal complexes for 2-amino-4-phenylthiazole derivative.

Abstract
This article describes the synthesis of novel bidentate Schiff base (H2L) from condensation of 2-amino-4-phenylthiazole (APT) with 4,6-diacetylresorcinol (DAR) in the molar ratio 2:1. We studied interaction of ligand (H2L) with transition metal ions such as Cr(III), Fe(III), Cu(II), Zn(II) and Cd(II). The ligand (H2L) has two bidentate sets of (N-O) units which can coordinate with two metal ions to afford novel binuclear metal complexes. The directions of coordinate bonds are from nitrogen atoms of azomethine groups and oxygen atoms of the phenolic groups. Structures of the newly synthesized complexes were confirmed by elemental analysis, IR, UV, (1)H NMR, ESR, TGA and mass spectral data. All of the newly synthesized complexes were evaluated for their antibacterial and anti-fungal activities. They were also evaluated for their in vitro anticancer activity against human colon carcinoma cells (HCT-116) and mammalian cells of African green monkey kidney (VERO). The Cu(II) complex with selectivity index (S.I.)=21.26 exhibited better activity than methotrexate (MTX) as a reference drug with S.I. value=13.30, while Zn(II) complex with S.I. value=10.24 was found to be nearly as active as MTX. Molecular docking studies further helped in understanding the mode of action of the compounds through their various interactions with active sites of dihydrofolate reductase (DHFR) enzyme. The observed activity of Fe(III) and Cu(II) complexes gave rise to the conclusion that they might exert their action through inhibition of the DHFR enzyme.
AuthorsSami A Al-Harbi, Mahmoud S Bashandy, Hammed M Al-Saidi, Adel A A Emara, Tarek A A Mousa
JournalSpectrochimica acta. Part A, Molecular and biomolecular spectroscopy (Spectrochim Acta A Mol Biomol Spectrosc) Vol. 145 Pg. 425-439 (Jun 15 2015) ISSN: 1873-3557 [Electronic] England
PMID25796013 (Publication Type: Journal Article)
CopyrightCopyright © 2015 Elsevier B.V. All rights reserved.
Chemical References
  • Anti-Bacterial Agents
  • Antineoplastic Agents
  • Coordination Complexes
  • Ligands
  • Metals
  • Schiff Bases
  • Thiazoles
  • phenthiazamine
  • Tetrahydrofolate Dehydrogenase
  • Methotrexate
Topics
  • Animals
  • Anti-Bacterial Agents (pharmacology)
  • Antineoplastic Agents (pharmacology, therapeutic use)
  • Bacteria (drug effects)
  • Catalytic Domain
  • Cell Death (drug effects)
  • Chlorocebus aethiops
  • Colonic Neoplasms (drug therapy, pathology)
  • Coordination Complexes (chemical synthesis, chemistry, pharmacology, therapeutic use)
  • Electron Spin Resonance Spectroscopy
  • Electrons
  • Fungi (drug effects)
  • HCT116 Cells
  • Humans
  • Ligands
  • Mass Spectrometry
  • Metals (pharmacology, therapeutic use)
  • Methotrexate (chemistry, pharmacology)
  • Microbial Sensitivity Tests
  • Molecular Docking Simulation
  • Proton Magnetic Resonance Spectroscopy
  • Schiff Bases (chemical synthesis, chemistry)
  • Spectrophotometry, Infrared
  • Tetrahydrofolate Dehydrogenase (chemistry)
  • Thermogravimetry
  • Thiazoles (chemical synthesis, chemistry, pharmacology, therapeutic use)
  • Vero Cells
  • Vibration

Join CureHunter, for free Research Interface BASIC access!

Take advantage of free CureHunter research engine access to explore the best drug and treatment options for any disease. Find out why thousands of doctors, pharma researchers and patient activists around the world use CureHunter every day.
Realize the full power of the drug-disease research graph!


Choose Username:
Email:
Password:
Verify Password:
Enter Code Shown: