Synthesis and cytotoxicity evaluation of thiophene analogues of 1-methyl-2,3-bis(hydroxymethyl)benzo[g]indole bis[N-(2-propyl)carbamate]

The cytotoxicity of the bis[N-(2-propyl)carbamates] 2 and 3 which are linked to thieno[i,j-g]indole scaffolds through methylene bridges were studied as thiopheric analogues of prototype 1. Compounds 2 and 3 were evaluated in vitro against 60 human-tumor cell lines derived from nine cancer-cell types and demonstrated, for compound 3 not only strong growth-inhibitory activities against leukemia cancer cells, but also fairly good activities against the growth of certain renal and ovarian cancer cell lines. Compound 2, the thieno[2,3-g]indole bis-carbamate, possessed only significant (MG-MID log(10) GI(50)= -4.89) and selective cytoxicity against NCI-HOP92 (non-small cell lung), MALME 3M (melanoma) and IGROV 1 (ovarian) cancer cell with log(10) GI(50) values of - 5.66, - 5.48 and - 5.47, respectively. (C) 2002 Editions scientifiques et medicales Elsevier SAS. All rights reserved.