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 thiophene 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 log10 GI50=−4.89) and selective cytoxicity against NCI–HOP92 (non-small cell lung), MALME 3M (melanoma) and IGROV 1 (ovarian) cancer cell with log10 GI50 values of −5.66, −5.48 and −5.47, respectively.