Novel and known analogs of thiocolchicine were evaluated in vitro in a tubulin binding assay and in vivo in mice for acute toxicity and in the P388 lymphocytic leukemia assay. Selected compounds also were investigated in the carrageenin-induced footpad edema in rate for antiinflammatory effects. A series of analogs of colchicide showed low tubulin binding affinity. An open-ring B analog of colchicine showed to tubulin binding affinity.