Synthesis and in vitro anticancer activity evaluation of biscarbamic esters of 2,3-bis(hydroxymethyl)-1-methyl-7- and 7,8-substituted-benzo[g]indoles.
A series of various bis(hydroxymethyl) carbamate derivatives of 7-mono- and 7,8-disubstituted-1-methyl-benzo[g]indoles was prepared in order to evaluate their cytostatic and cytotoxic activities in vitro. Compounds 2a-h showed significant tumor growth inhibition activity and were more potent than the 4,5-dihydrobenzo[g]indole analogues previously described. Compound 2a was the most active in this series, showing high activity and selectivity for some human cancer cell lines in the National Cancer Institute screen.
Pinna
G A
GA
Istituto di Chimica Farmaceutica e Tossicologica, Università di Sassari, Italy.
Pirisi
M A
MA
Sechi
M
M
Paglietti
G
G
D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D002219:Carbamates / Q000138:chemical synthesis* / Q000494:pharmacology; D006801:Humans; D007211:Indoles / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured
D000970:Antineoplastic Agents; D002219:Carbamates; D007211:Indoles