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.

Synthesis and cytotoxicity evaluation of thiophene analogues of 1-methyl-2,3-bis(hydroxymethyl)benzo[g]indole bis[N-(2-propyl)carbamate] / Pirisi, Maria Antonietta; Murineddu, Gabriele; Mussinu, J. M.; Pinna, Gerard Aime. - In: IL FARMACO. - ISSN 0014-827X. - 57:4(2002), pp. 331-335. [10.1016/S0014-827X(02)01201-6]

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

MURINEDDU, Gabriele;PINNA, Gerard Aime
2002-01-01

Abstract

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.
2002
Synthesis and cytotoxicity evaluation of thiophene analogues of 1-methyl-2,3-bis(hydroxymethyl)benzo[g]indole bis[N-(2-propyl)carbamate] / Pirisi, Maria Antonietta; Murineddu, Gabriele; Mussinu, J. M.; Pinna, Gerard Aime. - In: IL FARMACO. - ISSN 0014-827X. - 57:4(2002), pp. 331-335. [10.1016/S0014-827X(02)01201-6]
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11388/61061
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