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

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• 作者：Pirisi ; M.A. ; Murineddu ; G. ; Mussinu ; J.M. ; Pinna ; G.A.
• 关键词：Biscarbamates ; Thieno[i ; j-g]indoles ; Cytotoxicity
• 刊名：Il Farmaco
• 出版年：2002
• 出版时间：April 1, 2002
• 年：2002
• 卷：57
• 期：4
• 页码：331-335
• 全文大小：165 K

文摘

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 log₁₀GI₅₀