書誌事項
- タイトル別名
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- Synthesis and Conversion of Bongkrekic Acid and its Bioactivity
説明
<p>Bongkrekic acid (BKA), isolated from the bacterium Burkholderia gladioli, is an inhibitor of adenine nucleotide translocator in the mitochondria inner membrane, and is also a suppressor of apoptosis. Therefore, BKA is an important tool for the investigation of apoptosis as well as mitochondria. Herein, we summarize our total synthesis of BKA and its analogues, and their biological activities. The total synthesis was achieved by employing a three-component convergent strategy based on Julia-Kocienski olefination and Suzuki coupling. Torquoselective olefination with an ynolate was applied for the efficient construction of an unsaturated ester. Based on the total synthesis, various BKA analogues were prepared for structure-activity relationship studies, which indicated that the carboxylic acid moieties were essential for the biological activities of BKA. More readily available BKA analogues with potent biological activity were also developed. A brief summary of the novel biological activities is also provided.</p>
収録刊行物
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- 有機合成化学協会誌
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有機合成化学協会誌 80 (12), 1136-1148, 2022-12-01
公益社団法人 有機合成化学協会
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キーワード
詳細情報 詳細情報について
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- CRID
- 1390575805130934016
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- ISSN
- 18836526
- 00379980
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- 本文言語コード
- ja
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- データソース種別
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- JaLC
- Crossref
- KAKEN
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- 抄録ライセンスフラグ
- 使用不可