絞り込み

18390

広告

急性胆管炎に抗菌薬をどう選択する? (日経BP)

こんにちは、AST専従薬剤師として抗菌薬適正使用に携わっている柏原です。今回は、急性胆管炎に対する薬物治療の考え方や、実際のASTの関わりについて紹介したいと思...

  1. 最前線で新型コロナ対応に当たったキーパー...
  2. 薬局の待合にデジタルサイネージを設置! ...
  3. 夜間頻尿でベオーバが追加処方された患者 ...
  4. 環境負荷に懸念 データセンター、再エネ利...

ニュース一覧

Design, synthesis and biological evaluation of 2-arylaminopyrimidine derivatives bearing 1,3,8-triazaspiro[4,5]decan-4-one or piperidine-3-carboxamide moiety as novel Type-I ALK inhibitors.

著者 Miao X , Xing L , Guo M , Zhang H , Liu S , Yin S , Gong P , Zhang D , Zhai X
Bioorg Chem.2019 Nov 21 ; ():103456.
この記事をPubMed上で見るPubMedで表示
この記事をGoogle翻訳上で見る Google翻訳で開く

スターを付ける スターを付ける     (37view , 0users)

Full Text Sources

Aiming to develop novel Type-I inhibitors of ALK to overcome extensive resistance mutations, especially the L1196M mutation surrounding the ATP pocket, two series of 2-arylaminopyrimidine derivatives (11a-f and 22a-t) were designed based on scaffold hopping. The extensive structural elaboration discovered compound 22o which possessed excellent IC values of 0.06 and 0.23 μM against ALK-positive Karpas299 and H2228 cell lines, respectively. Meanwhile, 22o displayed encouraging inhibitory potency in the ALK (2.5 nM) and ALK (6.5 nM) enzymatic assays. Furthermore, the AO/EB and Hoechst 33258 assays illustrated 22o could induce cell apoptosis in a dose-dependent manner. Eventually, the molecular docking of 22o with ALK clearly presented the vital interactions within the active site, which was in accordance with Type-I inhibitor binding mode.
PMID: 31787343 [PubMed - as supplied by publisher]
印刷用ページを開く Endnote用テキストダウンロード