Synthesis and SAR study of novel 3,3-diphenyl-1,3-dihydroindol-2-one derivatives as potent eIF2·GTP·Met-tRNAiMet ternary complex inhibitors.

Denoyelle, Séverine; Chen, Ting; Yang, Hongwei; Chen, Limo; Zhang, Yingzhen; Halperin, José A; Aktas, Bertal H; Chorev, Michael

Denoyelle, Séverine; Chen, Ting; Yang, Hongwei; Chen, Limo; Zhang, Yingzhen; Halperin, José A; Aktas, Bertal H; Chorev, Michael.

Affiliation

Denoyelle S; Laboratory for Translational Research, Harvard Medical School, One Kendall Square, Building 600, 3rd Floor, Cambridge, MA 02139, USA.

Eur J Med Chem ; 69: 537-53, 2013 Nov.

Article in En | MEDLINE | ID: mdl-24095748

Subject(s)

Antineoplastic Agents/pharmacology; Eukaryotic Initiation Factor-2/antagonists & inhibitors; Guanosine Triphosphate/antagonists & inhibitors; Indoles/pharmacology; RNA, Transfer, Met/antagonists & inhibitors; Animals; Antineoplastic Agents/chemical synthesis; Antineoplastic Agents/chemistry; Cell Line, Tumor; Cell Proliferation/drug effects; Dose-Response Relationship, Drug; Drug Screening Assays, Antitumor; Eukaryotic Initiation Factor-2/metabolism; Guanosine Triphosphate/metabolism; Humans; Indoles/chemical synthesis; Indoles/chemistry; Mice; Molecular Structure; RNA, Transfer, Met/metabolism; Structure-Activity Relationship

Key words

3,3-Diaryloxindole derivatives; ISTFANUWXAQLTD-UHFFFAOYSA-N; Inhibition of cancer cell proliferation; Mechanistic assays; Ternary complex TC; Translation initiation TI

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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: RNA, Transfer, Met / Eukaryotic Initiation Factor-2 / Guanosine Triphosphate / Indoles / Antineoplastic Agents Type of study: Prognostic_studies Limits: Animals / Humans Language: En Journal: Eur J Med Chem Year: 2013 Document type: Article Affiliation country: United States Country of publication: France

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