Studies on Antitumor-active 2, 3-Dioxopiperazine Derivatives. IV. Synthesis and Structure-Antitumor Activity Relationship of 1-[4-(2-Pyridylamino) benzyl]-2, 3- …

…, C YOSHIDA, S MURAKAMI, R TAKENO…

Index: Hori; Yoshida; Murakami; Takeno; Kiba; Tsuda; Kishimoto; Saikawa Chemical and Pharmaceutical Bulletin, 1981 , vol. 29, # 6 p. 1594 - 1605

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Abstract

1-Benzyl-4-[4-(2-pyridylamino) benzyl]-2, 3-dioxopiperazine derivatives, which are antitumor agents of a new type, were synthesized and the structure-activity relationships were investigated. Furthermore, the antitumor activities of 2, 3-dioxopiperazine derivatives were compared with those of 2, 5-or 2, 6-dioxopiperazines. 1-[4-(5-Amino-6-chloro-2-pyridyl) aminobenzyl]-4-benzyl-2, 3-dioxopiperazine (3a) showed excellent in vitro and in vivo ...