SYNTHESIS, CYTOTOXICITY, ANTITUMOR-ACTIVITY AND SEQUENCE SELECTIVE BINDING OF 2 PYRAZOLE ANALOGS STRUCTURALLY RELATED TO THE ANTITUMOR AGENTS U-71,184 AND ADOZELESIN

Two pyrazole analogs structurally related to the antitumor agents adoz elesin and U-71,184 respectively were synthesized. By using a polymera se chain reaction approach, both compounds show selective binding to A + T rich sequences exactly as reference compound U-71,184. In in vitr o assays, against L1210 cell lines, both derivatives showed cytotoxici ty in the ph? range, values comparable with the natural target compoun d (+)-CC-1065. The most active compound showed very high antitumor act ivity in mice implanted with L1210 cells (ILS% 363).