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A series of novel 2,3-bis(hydroxymethyl)benzo[d]pyrrolo[2,1-b]-thiazoles and their bis(alkylcarbamate) derivatives were synthesized for antitumor evaluation.The preliminary antitumor studies reveal that bis(hydroxymethyl) and their bis(alkylcarbamate) derivatives show significant antitumor activity in inhibiting human leukemia and various solid tumor cell growth in vitro.