Grella, Giuseppe Enrico and Cabras, M. Cristina and Murineddu, Gabriele and Pau, Amedeo (2003) Synthesis and cytotoxicity of substituted 2-benzylnaphth[2,3-d]imidazoles. European Journal of Pharmaceutical Sciences, Vol. 20 (3), p. 267-272. ISSN 0928-0987. Article.
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Designed as a new series of so called “bivalent ligand” containing the proposed 2-benzylnaphthimidazole-type structure, a number of 2-benzylnaphth[2,3-d]imidazoles, bearing various substituents, have been prepared by a synthetic approach involving an heterocyclization of 2,3-diaminonaphthalene 4 with appropriate imidates 3 (for 1b–i) followed by alkylation (for 1j–l) with the desired alkylating agent. Compounds 1b–f, h–l were subjected to primary biological evaluation for cancer cell growth inhibition (one-dose, three-cell assay), and the four most active terms, 1c, h, i and j, were then evaluated for their cytotoxic profiles in the National Cancer Institute’s (NCI) human disease-oriented, 60 cell line, in vitro antitumor screening protocol. Among them, two compounds (1h and 1i) are the most representatives demonstrating not only high growth-inhibitory activities against some leukemia cancer cells, but also fairly good activities against the growth of certain cell lines of some solid tumors
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