Studies on antitumor-active 2,3-dioxopiperazine derivatives. IV. Synthesis and structure-antitumor activity relationship of 1-(4-(2-pyridylamino)benzyl)-2,3-dioxopiperazine derivatives.
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抄録
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 antitumor activities. The compound 3a was obtained by reduction of 1-benzyl-4-[4-(5-nitro-2-pyridyl)aminobenzyl]-2, 3-dioxopiperazine (2d) with Sn-conc. HCl or SnCl2-hydrogen chloride-MeOH. Reduction products of 2d obtained under different conditions are discussed.
収録刊行物
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- CHEMICAL & PHARMACEUTICAL BULLETIN
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CHEMICAL & PHARMACEUTICAL BULLETIN 29 (6), 1594-1605, 1981
公益社団法人 日本薬学会
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詳細情報
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- CRID
- 1390282679140338304
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- NII論文ID
- 110003633868
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- NII書誌ID
- AA00602100
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- ISSN
- 13475223
- 00092363
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- PubMed
- 7296715
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- 本文言語コード
- en
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- データソース種別
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- JaLC
- Crossref
- PubMed
- CiNii Articles
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- 抄録ライセンスフラグ
- 使用不可