TY - JOUR
T1 - N-substituted-2-butyl-5-chloro-3H-imidazole-4-carbaldehyde derivatives as anti-tumor agents against Ehrlich ascites tumor cells in vivo
AU - Anil Kumar, C.
AU - Nanjunda Swamy, S.
AU - Gaonkar, S. L.
AU - Basappa,
AU - Salimath, Bharathi P.
AU - Rangappa, Kanchugarakoppal S.
PY - 2007/5
Y1 - 2007/5
N2 - 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.
AB - 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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U2 - 10.2174/157340607780620699
DO - 10.2174/157340607780620699
M3 - Article
C2 - 17504198
AN - SCOPUS:34248674920
SN - 1573-4064
VL - 3
SP - 269
EP - 276
JO - Medicinal Chemistry
JF - Medicinal Chemistry
IS - 3
ER -