66938-75-8Relevant academic research and scientific papers
Synthesis, Tubulin Binding, Antineoplastic Evalutaion, and Structure-Activity Relationship of Oncodazole Analogues
Kruse, Lawrence I.,Ladd, David L.,Harrsch, Peter B.,McCabe, Francis L.,Mong, Shau-Ming,et al.
, p. 409 - 417 (2007/10/02)
n an attempt to identify a soluble oncodazole analogue that could be easily formulated, a series of substituted oncodazoles was synthesized and evaluated for tubulin binding affinity, in vitro cyctotoxicity against cultured mouse B-16 cells, and ability to prolong lifespan at the maximally tolerated dose in the P388 mouse leukemia model.Biological evaluation of all the isomeric methyloncodazoles demonstrated the thiophene 4'-position to be the only site of significant bulk tolerance, although substitution of this position with polar or charged functional groups abolished biological activity.Simple esters of the 4'-carboxymethyloncodazole were shown to have enhanched antitumor activity and tubulin binding affinity relative to oncodazole.Despite a failure of this study to identify a water-soluble oncodazole with antitumor activity, the structure-activity relationship developed led to a derivative with enhanced activity in the P388 leukemia model and facilitated the preparation of a biologically active photolabile analogue.
Synthesis and anthelminthic acitivity of alkyl-(5-acyl-1-benzimidazol-2-yl) carbamates
Raeymackers,Van Gelder,Roevens,Janssen
, p. 586 - 594 (2007/10/05)
A series of alkyl-(5-acyl-l-H-benzimidazol-2-yl)-carbamates were prepared and screened for anthelminthic activity. Some of them were found to be fully active at low, atoxic oral dose levels against gastro-intestinal nematodes. The activity against Syphacia muris and Strongyloides ratta is indicated. From these studies methyl (5-benzoyl-1-H-benzimidazol-2-yl) carbamate (mebendazole) and methyl [5-(4-fluorobenzoyl)-1-H-benzimidazol-2-yl]carbamate (flubendazole) were selected for detailed investigation.
