N-Substituted-2-butyl-5-chloro-3H-imidazole-4-carbaldehyde derivatives as anti-tumor agents against Ehrlich ascites tumor cells in vivo.
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.
Kumar
C Anil
CA
Department of Studies in Chemistry, University of Mysore, Manasagangothri, Mysore, India.
Swamy
S Nanjunda
SN
Gaonkar
S L
SL
Basappa
Salimath
Bharathi P
BP
Rangappa
Kanchugarakoppal S
KS
D000447:Aldehydes / Q000737:chemistry / Q000494:pharmacology*; D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry*; D017209:Apoptosis / Q000187:drug effects; D002286:Carcinoma, Ehrlich Tumor / Q000188:drug therapy*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D007093:Imidazoles / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D000447:Aldehydes; D000970:Antineoplastic Agents; D007093:Imidazoles