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Synthesis, cytotoxicity, antitumor activity and sequence selective binding of two pyrazole analogs structurally
P G Baraldi1, B Cacciari, R Romagnoli
1Dipartimento di Biochimica e Biologia Molecolare, Università di Ferrara, Italy. pgb@dns.unife.it
Anti-Cancer Drug Design
|November 20, 1997
Abstract:
Two pyrazole analogs structurally related to the antitumor agents adozelesin and U-71,184 respectively were synthesized. By using a polymerase chain reaction approach, both compounds show selective binding to A + T rich sequences exactly as reference compound U-71,184. In in vitro assays, against L1210 cell lines, both derivatives showed cytotoxicity in the pM range, values comparable with the natural target compound (+)-CC-1065. The most active compound showed very high antitumor activity in mice implanted with L1210 cells (ILS% 363).