Novel inhibitors of epidermal growth factor receptor: (4-(Arylamino)-7H- pyrrolo[2,3-d]pyrimidin-6-yl)(1H-indol-2-yl)methanones and (1H-indol-2-yl)(4- (phenylamino)thieno[2,3-d]pyrimidin-6-yl)methanones

Bioorganic and Medicinal Chemistry

Volumn 20, Issue 1, 2012, Pages 125-136

  Beckers, Thomas ^e   Sellmer, Andreas ^a   Eichhorn, Emerich ^a   Pongratz, Herwig ^a   Schächtele, Christoph ^b   Totzke, Frank ^b   Kelter, Gerhard ^c   Krumbach, Rebekka ^c   Fiebig, Heinz Herbert ^c   Böhmer, Frank D ^d   Mahboobi, Siavosh ^a  

^a UNIVERSITY OF REGENSBURG   (Germany)

^b PROQINASE GMBH   (Germany)

^c CHARLES RIVER LABORATORIES   (United States)

^d JENA UNIVERSITY HOSPITAL   (Germany)

^e NONE

Author keywords

Anticancer agents; Bisindolylmethanone; Epidermal growth factor receptor (EGFR); Quinazoline; Tyrosine kinase inhibitor

Indexed keywords

(1H INDOL 2 YL)[4 (3 IODOPHENYLAMINO) 7H PYRROLO[2,3 D]PYRIMIDIN 6 YL]METHANONE; (1H INDOL 2 YL)[4 (PHENYLAMINO) 1H INDOL 2 YL]METHANONE DERIVATIVE; (1H INDOL 2 YL)[4 (PHENYLAMINO)THIENO[2,3 D]PYRIMIDIN 6 YL]METHANONE DERIVATIVE; (4 CHLOROBENZO[B]THIOPHEN 2 YL)[1 (PHENYLSULFONYL) 1H INDOL 2 YL]METHANONE DERIVATIVE; (4 CHLOROTHIENO[2,3 D]PYRIMIDIN 6 YL)[1 (PHENYLSULFONYL) 1H INDOL 2 YL]METHANONE; (4 CHLOROTHIENO[2,3 D]PYRIMIDIN 6 YL)[5 METHOXY 1 (PHENYLSULFONYL) 1H INDOL 2 YL]METHANONE; 1 (PHENYLSULFONYL) 1H PYRROLO[2,3 B]PYRIDINE; 4 CHLORO 7 (PHENYLSULFONYL) 7H PYRROLO[2,3 D]PYRIMIDINE; 4 CHLORO 7 (PHENYLSULFONYL) 7H PYRROLO[2,3 D]PYRIMIDINE 6 CARBONYL CHLORIDE; 4 CHLORO 7 (PHENYLSULFONYL) 7H PYRROLO[2,3 D]PYRIMIDINE 6 CARBOXYLIC ACID; 4 CHLOROTHIENO[2,3 D]PYRIMIDINE 6 CARBONYL CHLORIDE; 4 CHLOROTHIENO[2,3 D]PYRIMIDINE 6 CARBOXYLIC ACID; 6 (4 HYDROXYPHENYL) 4 (ALPHA METHYLBENZYLAMINO) 7H PYRROLO[2,3 D]PYRIMIDINE; [4 (3 CHLORO 4 FLUOROPHENYLAMINO) 7H PYRROLO[2,3 D]PYRIMIDIN 6 YL](1H INDOL 2 YL)METHANONE; [4 (3 ETHYNYLPHENYLAMINO) 7H PYRROLO[2,3 D]PYRIMIDIN 6 YL](1H INDOL 2 YL)METHANONE; [4 (4 CHLOROPHENYLAMINO) 7H PYRROLO[2,3 D]PYRIMIDIN 6 YL](1H INDOL 2 YL)METHANONE; [4 (ARYLAMINO) 7H PYRROLO[2,3 D]PYRIMIDIN 6 YL](1H INDOL 2 YL)METHANONE DERIVATIVE; [4 CHLORO 7 (PHENYLSULFONYL) 7H PYRROLO[2,3 D]PYRIMIDIN 6 YL][1 (PHENYLSULFONYL) 1H INDOL 2 YL]METHANONE DERIVATIVE; [4 CHLORO 7 (PHENYLSULFONYL) 7H PYRROLO[2,3 D]PYRIMIDIN 6 YL][1 (PHENYLSULFONYL) 1H PYRROLO[2,3 B]PYRIDINE 2 YL]METHANONE; [4 CHLORO 7 (PHENYLSULFONYL) 7H PYRROLO[2,3 D]PYRIMIDIN 6 YL][5 METHOXY 1 (PHENYLSULFONYL) 1H INDOL 2 YL]METHANONE; [5 (BENZYLOXY) 1 (PHENYLSULFONYL) 1H INDOL 2 YL][4 CHLORO 7 (PHENYLSULFONYL) 7H PYRROLO[2,3 D]PYRIMIDIN 6 YL]METHANONE; [5 (TERT BUTYLDIMETHYLSILYLOXY) 1 (PHENYLSULFONYL) 1H INDOL 2 YL](4 CHLOROTHIENO[2,3 D]PYRIMIDIN 6 YL)METHANONE; ANTINEOPLASTIC AGENT; EPIDERMAL GROWTH FACTOR RECEPTOR; ERLOTINIB; GEFITINIB; LAPATINIB; TANDUTINIB; UNCLASSIFIED DRUG; UNINDEXED DRUG; VANDETANIB;

ANTINEOPLASTIC ACTIVITY; ARTICLE; CANCER CELL; CARBOXYLATION; CONTROLLED STUDY; DRUG EFFICACY; DRUG POTENCY; DRUG SCREENING; DRUG STRUCTURE; DRUG SYNTHESIS; DRUG TOLERABILITY; ENZYME INHIBITION; HUMAN; HUMAN CELL; IC 50; LIPOPHILICITY; PROTEIN PHOSPHORYLATION;

ANTINEOPLASTIC AGENTS; CELL LINE, TUMOR; DRUG SCREENING ASSAYS, ANTITUMOR; HUMANS; INDOLES; PHOSPHORYLATION; PYRIMIDINES; QUINAZOLINES; RECEPTOR, EPIDERMAL GROWTH FACTOR; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84855187986     PISSN: 09680896     EISSN: 14643391     Source Type: Journal    
DOI: 10.1016/j.bmc.2011.11.023     Document Type: Article

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