14294-12-3Relevant academic research and scientific papers
Benzothiazole thiourea derivatives as anticancer agents: Design, synthesis, and biological screening
Eshkil, Fatemeh,Eshghi, Hossein,Saljooghi, Amir. Sh.,Bakavoli, Mehdi,Rahimizadeh, Mohammad
, p. 576 - 582 (2017)
In a systematic effort to identify a potent anticancer agent, we synthesized benzothiazole thiourea derivatives and examined their cytotoxic activity against five different human and animal cancer cell lines. Benzothiazolylthiocarbamides have been prepared in excellent yields by reaction of substituted 2-amino benzothiazoles with carbon disulfide and dimethyl sulfate followed by their ammonolysis. Cytotoxicity of the four compounds were screened for antitumor activity against human breast cancer cells (MCF-7), human cervix epithelial carcinoma (HeLa), human colon cancer cell line (HT-29), human leukemia cell line (K-562), and mouse neuroblastoma cell line (Neuro-2a) using cisplatin as a reference by MTT assay. Our results presented herein provide experimental evidence that benzothiazolylthiocarbamides induce apoptosis in cancer cell lines. According to flow cytometry results, treatment of HT-29 cells with 1-(6-ethoxy-1,3-benzothiazol- 2-yl)thiourea produced a large population of apoptotic cell (79.45%), which was 1.2-fold higher than that produced by cisplatin (65.28%) at the same concentration.
OPIOID RECEPTOR MODULATORS AND USE THEREOF
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, (2017/03/21)
Disclosed is an in vitro screening method for identifying an antagonist-to-agonist allosteric modifier of a mu-opioid receptor and an in vivo method for confirming that a test compound is such a modifier of a mu-opioid receptor. Also disclosed is a method
Synthesis, characterization and studies on antioxidant and molecular docking of metal complexes of 1-(benzo[d]thiazol-2-yl)thiourea
Yapati, Harinath,Devineni, Subba Rao,Chirumamilla, Suresh,Kalluru, Seshaiah
, p. 43 - 51 (2016/02/09)
In the present study, a new thiourea derivative bearing benzothiazole ligand, 1-(benzo[d]thiazol-2-yl)thiourea (btt) and its ternary metal (Cu(II), Co(II) and Ni(II)) complexes were synthesized. The structural characterization was carried out by micro analysis, IR, 1H-NMR, EPR, UV-Visible spectral analyses, molar conductance and thermal analysis studies. Spectral studies of complexes revealed that the metal complexes have distorted octahedral geometry. Molecular modelling study was performed to evaluate the recognition of target compounds at the 3MNG binding pocket. The docking results revealed that copper complex selectively binds to the crucial amino acid residues in the active site of 3MNG. The in vitro antioxidant activity of the ligand and its metal complexes was assayed by radical scavenging activity (DPPH, H2O2 and NO) and ferric reducing antioxidant power (FRAP) methods. The ligand showed moderate antioxidant activity whereas the metal complexes exhibited better antioxidant activity than that of the ligand. The results of the four methods proved that the copper complex is the most potent antioxidant among all the tested compounds.
Pyrimidinone antibiotics - Heterocyclic analogues with improved antibacterial spectrum
Brands, Michael,Grande, Yolanda Cancho,Endermann, Rainer,Gahlmann, Reinhold,Krueger, Jochen,Raddatz, Siegfried
, p. 2641 - 2645 (2007/10/03)
We report the synthesis and pharmacological evaluation of new derivatives of the natural dipeptide antibiotic TAN 1057 A,B containing heterocycles either in the β-amino acid side chain or as mimics of the urea function. In the course of this program, we identified novel analogues that display activity towards a broader panel of Gram-positive bacteriae.
