当前位置： SCI文献检索 > EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY期刊下所有文献 > Synthesis and biological evaluation of novel 2-aralkyl-5-substituted-6-(4'-fluorophenyl)-imidazo[2,1-b][1,3,4]thiadiazole derivatives as potent anticancer agents.

Synthesis and biological evaluation of novel 2-aralkyl-5-substituted-6-(4'-fluorophenyl)-imidazo[2,1-b][1,3,4]thiadiazole derivatives as potent anticancer agents.

Abstract：

:Levamisole, the imidazo[2,1-b]thiazole derivative has been reported as a potential antitumor agent. In the present study, we synthesized, characterized and evaluated biological activity of its novel analogues with substitution in the aralkyl group and on imidazothiadiazole molecules with same chemical backbone but different side chains namely 2-aralkyl-6-(4'-fluorophenyl)-imidazo[2,1-b][1,3,4]thiadiazoles (SCR1), 2-aralkyl-5-bromo-6-(4'-fluorophenyl)-imidazo[2,1-b][1,3,4]-thiadiazoles (SCR2), 2-aralkyl-5-formyl-6-(4'-fluorophenyl)-imidazo[2,1-b][1,3,4]-thiadiazoles (SCR3) and 2-aralkyl-5-thiocyanato-6-(4'-fluorophenyl)-imidazo[2,1-b][1,3,4]-thiadiazoles (SCR4) on leukemia cells. The cytotoxic studies showed that 3a, 4a, and 4c exhibited strong cytotoxicity while others had moderate cytotoxicity. Among these we chose 4a (IC50, 8 μM) for understanding its mechanism of cytotoxicity. FACS analysis in conjunction with mitochondrial membrane potential and DNA fragmentation studies indicated that 4a induced apoptosis without cell cycle arrest suggesting that it could be used as a potential chemotherapeutic agent.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Karki SS,Panjamurthy K,Kumar S,Nambiar M,Ramareddy SA,Chiruvella KK,Raghavan SC

doi

10.1016/j.ejmech.2011.02.064

subject

Has Abstract

pub_date

2011-06-01 00:00:00

pages

2109-16

issue

6

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(11)00192-9

journal_volume

46

pub_type

杂志文章

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