205051-29-2Relevant academic research and scientific papers
Synthesis and antitumor activity of duocarmycin derivatives: Modification at the C-7 position of segment-A of A-ring pyrrole compounds
Amishiro, Nobuyoshi,Okamoto, Akihiko,Okabe, Masami,Saito, Hiromitsu
, p. 1195 - 1201 (2000)
A series of the C7-substituted A-ring pyrrole derivatives of duocarmycin were synthesized, and evaluated for in vitro anticellular activity against HeLa S3 cells and in vivo antitumor activity against murine sarcoma 180 in mice. All of the C7-substituted A-ring pyrrole compounds decreased potency in vitro and in vivo. However, some showed strong antitumor activity with T/C values less than 0.3. Among them, the 7-formyl compound 5d showed remarkable potent in vivo antitumor activity and low peripheral blood toxicity, which were equal to 2c. (C) 2000 Elsevier Science Ltd.
