Abstract
Quinoxaline-2, 3-dione obtained from cyclocondensation reaction of o-phenylene diamine with oxalic acid, was reacted with chlorosulphonic acid under cold condition followed by a reaction with various benzimidazoles to give 2, 3- dioxo-1, 2, 3, 4-tetrahydroquinoxaline-6-sulphonyl benzimidazoles in satisfactory yield. Their structures were confirmed using 1H NMR, IR and mass analysis. Cytotoxicity of these derivatives were evaluated by growth inhibition of HEp-2 cells in vitro. The preliminary bioassay indicated that these compounds showed moderate cytotoxicity.
Keywords: Benzimidazole, Cytotoxicity, Quinoxaline-2,3-dione, SRB method, Electrophilic substitution, Human epithelial carcinoma cell line, Hetrocycles, Organic Synthesis, Antimalarial Activities, Benzimidazole Derivatives, Pharmacological Activities, Anthelminitic Agents, Veterinarian Medicine, Human Therapeutic Areas, Oxalic acid Dihydrate, Catalyst Microwave System
Letters in Drug Design & Discovery
Title: Synthesis and Characterization of some Novel Quinoxaline-2, 3-Dione Derivatives: A Preliminary Investigation on their Activity Against a Human Epithelial Carcinoma Cell Line
Volume: 8 Issue: 4
Author(s): Selvaraj Jubie, Rajamanickam Gayathri, Ammayappan Rajam Srividya, Rajagopal Kalirajan, Prabakaran Prabitha, Sundaram Sankar and Kannan Elango
Affiliation:
Keywords: Benzimidazole, Cytotoxicity, Quinoxaline-2,3-dione, SRB method, Electrophilic substitution, Human epithelial carcinoma cell line, Hetrocycles, Organic Synthesis, Antimalarial Activities, Benzimidazole Derivatives, Pharmacological Activities, Anthelminitic Agents, Veterinarian Medicine, Human Therapeutic Areas, Oxalic acid Dihydrate, Catalyst Microwave System
Abstract: Quinoxaline-2, 3-dione obtained from cyclocondensation reaction of o-phenylene diamine with oxalic acid, was reacted with chlorosulphonic acid under cold condition followed by a reaction with various benzimidazoles to give 2, 3- dioxo-1, 2, 3, 4-tetrahydroquinoxaline-6-sulphonyl benzimidazoles in satisfactory yield. Their structures were confirmed using 1H NMR, IR and mass analysis. Cytotoxicity of these derivatives were evaluated by growth inhibition of HEp-2 cells in vitro. The preliminary bioassay indicated that these compounds showed moderate cytotoxicity.
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Jubie Selvaraj, Gayathri Rajamanickam, Rajam Srividya Ammayappan, Kalirajan Rajagopal, Prabitha Prabakaran, Sankar Sundaram and Elango Kannan, Synthesis and Characterization of some Novel Quinoxaline-2, 3-Dione Derivatives: A Preliminary Investigation on their Activity Against a Human Epithelial Carcinoma Cell Line, Letters in Drug Design & Discovery 2011; 8 (4) . https://dx.doi.org/10.2174/157018011794839385
DOI https://dx.doi.org/10.2174/157018011794839385 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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