Synthesis and RET protein kinase inhibitory activity of 3-arylureidobenzylidene-indolin-2-ones

Bioorganic and Medicinal Chemistry Letters

Volumn 17, Issue 14, 2007, Pages 3962-3968

  Rizzi, Eleonora ^a   Cassinelli, Giuliana ^b   Dallavalle, Sabrina ^a   Lanzi, Cinzia ^b   Cincinelli, Raffaella ^a   Nannei, Raffaella ^a   Cuccuru, Giuditta ^b   Zunino, Franco ^b  

^a UNIVERSITY OF MILAN   (Italy)

^b Dipto di Oncologia Sperimentale   (Italy)

Author keywords

Antitumour; Indolinone; Protein kinase; RET; Synthesis; Thyroid cancer

Indexed keywords

5,6 DIMETHOXYINDOLINONE DERIVATIVE; ENZYME INHIBITOR; INDOLE DERIVATIVE; PROTEIN RET; PROTEIN RET INHIBITOR; RPI 1; UNCLASSIFIED DRUG; UREIDOBENZYLIDENEINDOLIN 2 ONE DERIVATIVE;

ANIMAL CELL; ARTICLE; CELL CULTURE; CELL STRAIN 3T3; CONTROLLED STUDY; CULTURE MEDIUM; DRUG STRUCTURE; DRUG SYNTHESIS; ENZYME ACTIVITY; ENZYME INHIBITION; HYDROGENATION; IC 50; MOUSE; NONHUMAN; ONCOGENE; PHENOTYPE; POLYMERIZATION; REACTION ANALYSIS; STRUCTURE ACTIVITY RELATION; STRUCTURE ANALYSIS; WESTERN BLOTTING;

ANIMALS; BLOTTING, WESTERN; INDOLES; MICE; NIH 3T3 CELLS; PROTEIN KINASE INHIBITORS; PROTO-ONCOGENE PROTEINS C-RET; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 34250316191     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2007.04.091     Document Type: Article

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27. 20 The following antibodies were used: monoclonal anti-pTyr antibody clone 4G10 (Upstate Biotechnology, Lake Placid, NY); rabbit polyclonal anti-Ret H300 and anti-pRet (Tyr1062) (Santa Cruz Biotechnology, Santa Cruz, CA) and anti-tubulin (Sigma Chemical Company, St. Louis, MO).
28. 4 and 0.18 mM dithiothreitol) with solvent or inhibitor (DMSO 4% final concentration) in the presence of 2 μM MBP and 5 μM ATP. The reaction was stopped by 3-fold concentrated Laemmli buffer, then samples were subjected to SDS-PAGE and immunoblotted with anti-pTyr antibody. Phosphorylated MBP was revealed by chemioluminescence reaction ECL (GE Healthcare, Little Chalfont, UK) and detected by ChemiDoc XRS System, PC. Signal intensity was analyzed with the interfaced software Quantity One 4.6.3 (Bio-Rad, Hercules, CA).