Synthesis of Some Benzothiazole Based Piperazine-Dithiocarbamate Derivatives and Evaluation of Their Anticancer Activities
31 Oct 2011-Letters in Drug Design & Discovery (Bentham Science Publ LTD)-Vol. 8, Iss: 9, pp 830-837
About: This article is published in Letters in Drug Design & Discovery.The article was published on 2011-10-31. It has received 12 citations till now. The article focuses on the topics: Benzothiazole & Dithiocarbamate.
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TL;DR: Donepezil (DNP), an acetylcholinesterase (AChE) inhibitor, is one of the most preferred choices in Alzheimer diseases (AD) therapy and 38 new DNP analogues were synthesized.
71 citations
TL;DR: Results provide promising starting points for further development of novel kinase inhibitors and highlight the anchoring role of the nitrothiazole moiety in bonding and hydrophobic interaction with the key amino acid residues.
Abstract: In an attempt to develop potent antitumor agents, new 1,3,4-thiadiazole derivatives were synthesized and evaluated for their cytotoxic effects on multiple human cancer cell lines, including the K562 chronic myelogenous leukemia cell line that expresses the Bcr-Abl tyrosine kinase. N-(5-Nitrothiazol-2-yl)-2-((5-((4-(trifluoromethyl)phenyl)amino)-1,3,4-thiadiazol-2-yl)thio)acetamide (2) inhibited the Abl protein kinase with an IC50 value of 7.4 µM and showed selective activity against the Bcr-Abl positive K562 cell line. Furthermore, a Bcr-Abl-compound 2 molecular modelling simulation highlighted the anchoring role of the nitrothiazole moiety in bonding and hydrophobic interaction with the key amino acid residues. These results provide promising starting points for further development of novel kinase inhibitors.
41 citations
TL;DR: In this article, the role and importance of nitrogen-based heterocyclics in the development of antidepressant compounds has been highlighted, and a review focusing on the selection of these heter-ocyclic moieties for the further design and development of promising antidepressants by taking a clue from the earlier reported potent antidepressant compounds or from the marketed products.
29 citations
TL;DR: Flow cytometry analysis showed that compounds 4a-4p have a remarkable anticancer activity and a good selectivity towards C6 cell lines and that these compounds display antic cancer activity by inducing apoptosis.
Abstract: Sixteen new 2-(benzothiazol-2-ylthio)-N′-(3-substituted-4-(3,4-substitutedphenyl)thiazol-2(3H)-ylidene)acetohydrazide derivatives (4a-4p) were synthesized. The structures of the synthesized compoun...
27 citations
TL;DR: The obtained results showed that compounds 3c, 3d, 3f–3h reduced the immobility time of mice as assessed in the tail suspension test and increased the swimming frequencies of mice, without any alteration in the climbing frequencies.
Abstract: Within the scope of our new antidepressant drug development efforts, in this study, we synthesized eight novel benzothiazole derivatives 3a–3h. The chemical structures of the synthesized compounds were elucidated by spectroscopic methods. Test compounds were administered orally at a dose of 40 mg/kg to mice 24, 5 and 1 h before performing tail suspension, modified forced swimming, and activity cage tests. The obtained results showed that compounds 3c, 3d, 3f–3h reduced the immobility time of mice as assessed in the tail suspension test. Moreover, in the modified forced swimming tests, the same compounds significantly decreased the immobility, but increased the swimming frequencies of mice, without any alteration in the climbing frequencies. These results, similar to the results induced by the reference drug fluoxetine (20 mg/kg, po), indicated the antidepressant-like activities of the compounds 3c, 3d, 3f–3h. Owing to the fact that test compounds did not induce any significant alteration in the total number of spontaneous locomotor activities, the antidepressant-like effects of these derivatives seemed to be specific. In order to predict ADME parameters of the synthesized compounds 3a–3h, some physicochemical parameters were calculated. The ADME prediction study revealed that all synthesized compounds may possess good pharmacokinetic profiles.
25 citations