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- l-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.