Abstract
A new series of N-substituted 2-butyl-5-chloro-3H-imidazole-4-carbaldehyde derivatives were synthesized by using the different bioactive heteroaralkyl halides with 2-butyl-4-chloro-1H-imidazole-5-carbaldehyde in presence of powdered potassium carbonate in DMF medium. These compounds were screened for their antitumor activity. Our results show that treatment of imidazole derivatives inhibit proliferation EAT cells, decreases the ascites volume and increases the survivability of the animals in vivo. These compounds also inhibited the cellular proliferation of HUVEC cells in vitro by MTT assay. Further, these compounds could induce apoptosis, which is evident by the nuclear condensation of imidazole derivatives treated EAT cells in vivo by the cytological analysis. We have identified that pyrrolidine substituted imidazole derivative as potent anti-tumor compound. These inhibitors could represent as promising candidates for anticancer therapies, where the formation of peritoneal malignant ascites is a major cause of morbidity and mortality.
Keywords: Antitumor activity, HUVEC, imidazole derivative, EAT cells
Medicinal Chemistry
Title: N-Substituted-2-butyl-5-chloro-3H-imidazole-4-carbaldehyde Derivatives as Anti-tumor Agents Against Ehrlich Ascites tumor Cells In Vivo
Volume: 3 Issue: 3
Author(s): C. Anil Kumar, S. Nanjunda Swamy, S. L. Gaonkar, Basappa, Bharathi P. Salimath and Kanchugarakoppal S. Rangappa
Affiliation:
Keywords: Antitumor activity, HUVEC, imidazole derivative, EAT cells
Abstract: A new series of N-substituted 2-butyl-5-chloro-3H-imidazole-4-carbaldehyde derivatives were synthesized by using the different bioactive heteroaralkyl halides with 2-butyl-4-chloro-1H-imidazole-5-carbaldehyde in presence of powdered potassium carbonate in DMF medium. These compounds were screened for their antitumor activity. Our results show that treatment of imidazole derivatives inhibit proliferation EAT cells, decreases the ascites volume and increases the survivability of the animals in vivo. These compounds also inhibited the cellular proliferation of HUVEC cells in vitro by MTT assay. Further, these compounds could induce apoptosis, which is evident by the nuclear condensation of imidazole derivatives treated EAT cells in vivo by the cytological analysis. We have identified that pyrrolidine substituted imidazole derivative as potent anti-tumor compound. These inhibitors could represent as promising candidates for anticancer therapies, where the formation of peritoneal malignant ascites is a major cause of morbidity and mortality.
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Cite this article as:
Anil Kumar C., Nanjunda Swamy S., Gaonkar L. S., Basappa , Salimath P. Bharathi and Rangappa S. Kanchugarakoppal, N-Substituted-2-butyl-5-chloro-3H-imidazole-4-carbaldehyde Derivatives as Anti-tumor Agents Against Ehrlich Ascites tumor Cells In Vivo, Medicinal Chemistry 2007; 3 (3) . https://dx.doi.org/10.2174/157340607780620699
DOI https://dx.doi.org/10.2174/157340607780620699 |
Print ISSN 1573-4064 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6638 |
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