Discovery of Chromeno[4,3-c]pyrazol-4(2H)-one Containing Carbonyl or Oxime Derivatives as Potential, Selective Inhibitors PI3Kα
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- Lu Liang
- State Key Laboratory of Pharmaceutical Biotechnology, Nanjing University
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- Sha Shao
- State Key Laboratory of Pharmaceutical Biotechnology, Nanjing University
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- Wang Kai
- State Key Laboratory of Pharmaceutical Biotechnology, Nanjing University
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- Zhang Yuan-Heng
- State Key Laboratory of Pharmaceutical Biotechnology, Nanjing University
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- Liu Yan-Dong
- State Key Laboratory of Pharmaceutical Biotechnology, Nanjing University
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- Ju Guo-Dong
- State Key Laboratory of Pharmaceutical Biotechnology, Nanjing University
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- Wang Baozhong
- State Key Laboratory of Pharmaceutical Biotechnology, Nanjing University
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- Zhu Hai-Liang
- State Key Laboratory of Pharmaceutical Biotechnology, Nanjing University
書誌事項
- タイトル別名
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- Discovery of Chromeno[4,3-<i>c</i>]pyrazol-4(2<i>H</i>)-one Containing Carbonyl or Oxime Derivatives as Potential, Selective Inhibitors PI3Kα
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<p>A series of novel chromeno[4,3-c]pyrazol-4(2H)-one containing carbonyl or oxime derivatives (4a–n, 5a–n) have been synthesized and evaluated their biological activities as phosphatidyl inositol 3-kinase (PI3K) inhibitors. Out of them, compound 5l showed the most potent antiproliferative activities against HCT-116 with IC50 of 0.10 µM in vitro, and exhibited the most potent activity for PI3Kα with the value of 0.012 µM. Docking simulation of 5l into PI3Kα active site were performed to determine the probable binding model, and it indicated that compound 5l could be optimized as a potential inhibitor of PI3Kα in the further study.</p>
収録刊行物
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- CHEMICAL & PHARMACEUTICAL BULLETIN
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CHEMICAL & PHARMACEUTICAL BULLETIN 64 (11), 1576-1581, 2016
公益社団法人 日本薬学会
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詳細情報 詳細情報について
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- CRID
- 1390282679155748864
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- NII論文ID
- 130005268017
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- NII書誌ID
- AA00602100
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- ISSN
- 13475223
- 00092363
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- NDL書誌ID
- 027684651
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- PubMed
- 27581755
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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
- NDL
- Crossref
- PubMed
- CiNii Articles
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- 抄録ライセンスフラグ
- 使用不可