16730-20-4Relevant academic research and scientific papers
Preparation of 5-substituted 2-carboxyindoles on solid support
Tois, Jan,Franzén, Robert,Aitio, Olli,Huikko, Katri,Taskinen, Jyrki
, p. 2443 - 2446 (2000)
The preparation of 5-substituted 2-carboxyindoles on solid support is reported. In the approach, the indole moiety is synthesized in solution phase, followed by nitro-group reduction, reductive amination and alkylation on solid support. The method provides a simple and convenient route for the preparation of 5-substituted 2-carboxyindoles with high purity and good yield. (C) 2000 Elsevier Science Ltd.
Oligomer modified diaromatic substituted compounds
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, (2016/01/30)
Disclosed are compounds comprising diaromatic substituted compound residues, namely the anti-viral (anti-HIV) drug delavirdine, covalently attached via a linkage to water-soluble, non-peptidic oligomers, specifically to poly(ethylene glycol) (PEG) oligome
Indole-2-acetamide compound with anti-inflammatory effect, and application thereof in preparation of anti-inflammatory drugs
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Paragraph 0051; 0053, (2016/10/27)
The invention discloses an indole-2-acetamide compound with an anti-inflammatory effect, and an application thereof in preparation of anti-inflammatory drugs. The indole-2-amide compound is represented by one of formula (I) to formula (III), and in the fo
Synthesis and biological evaluation of antibody conjugates of phosphate prodrugs of cytotoxic DNA alkylators for the targeted treatment of cancer
Zhao, Robert Yongxin,Erickson, Hans K.,Leece, Barbara A.,Reid, Emily E.,Goldmacher, Victor S.,Lambert, John M.,Chari, Ravi V. J.
experimental part, p. 766 - 782 (2012/03/11)
The synthesis and biological evaluation of phosphate prodrugs of analogues of 1 (CC-1065) and their conjugates with antibodies are described. The phosphate group on the 1,2,9,9a-tetrahydrocyclopropa[c]benz[e]indol-4-one (CBI) portion of the compounds conf
Structural influence of indole C5-N-substitutents on the cytotoxicity of seco-duocarmycin analogs
Choi, Taeyoung,Ma, Eunsook
experimental part, p. 357 - 367 (2012/05/04)
A series of racemic indole C5-substituted seco-cyclopropylindoline compounds (2,3 and 5-7) were prepared by coupling 1-(tert-butyloxycarbonyl)-3- (chlorocarbonyl)indoline (seg-A) with 5,6,7-trimethoxy-, 5,6-dimethoxy-, 5-amino-, 5-methylsulfonylamino- and 5-(N,N-dimethylaminosulfonylamino) indole-2-carboxylic acid as seg-B in the presence of 1-ethyl-3-(3- dimethylaminopropyl) carbodiimide. The synthetic compounds (2,3 and 5-7) were tested for cytotoxic activity against human cancer cell lines (COLO 205, SK-MEL-2, A549, and JEG-3) using the MTT assay.
Synthesis and evaluation of a series of C5′-substituted duocarmycin SA analogs
Robertson, William M.,Kastrinsky, David B.,Hwang, Inkyu,Boger, Dale L.
body text, p. 2722 - 2725 (2011/07/06)
The synthesis and evaluation of a key series of analogs of duocarmycin SA, bearing a single substituent at the C5′ position of the DNA binding subunit, are described.
3,4-DIHYDRO-2H-PYRAZINO[1,2-A]INDOL-1-ONE DERIVATIVES ACTIVE AS KINASE INHIBITORS, PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS COMPRISING THEM
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Page/Page column 37, (2009/10/22)
Compounds which are 3,4-dihydro-2H-pyrazino[1,2-a]indol-1-one derivatives or pharmaceutically acceptable salts thereof,their preparation process and pharmaceutical compositions comprising them are disclosed; these compounds are useful in the treatment ofd
HETEROCYCLIC DERIVATIVES FOR MODULATION OF CALCIUM CHANNELS
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Page/Page column 221, (2008/06/13)
Heterocyclic derivatives act as Ca channel antagonists. The compositions are useful for treating or relieving Ca channel mediated conditions.
AMINOMETHYL SUBSTITUTED BICYCLIC AROMATIC COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF THE DOPAMINE D3 RECEPTOR
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Page/Page column 99, (2010/11/08)
The present invention relates to an aminomethyl substituted bicyclic aromatic compound of the formula (I) wherein Ar is a cyclic radical selected from the group consisting of phenyl, a 5- or 6-membered C-bound heteroaromatic radical comprising as ring mem
Sequence-specific alkylation of double-strand human telomere repeat sequence by pyrrole-imidazole polyamides with indole linkers
Sasaki, Shunta,Bando, Toshikazu,Minoshima, Masafumi,Shimizu, Tatsuhiko,Shinohara, Ken-Ichi,Takaoka, Toshiyasu,Sugiyama, Hiroshi
, p. 12162 - 12168 (2007/10/03)
We designed and synthesized pyrrole (Py)-imidazole (Im) hairpin polyamide 1-(chloromethyl)-5-hydroxy-1,2-dihydro-3H-benz[e]indole (seco-CBI) conjugates 1 and 2, which target both strands of -the double-stranded region of the human telomere repeat sequences, 5′-d(TTAGGG)n-3′/5′- d(CCCTAA)n-3′. High-resolution denaturing polyacrylamide gel electrophoresis demonstrated that conjugates 1 and 2 alkylated DNA at the 3′ A of 5′-ACCCTA-3′ and 5′-AGGGTTA-3′, respectively. Cytotoxicities of conjugates 1 and 2 were evaluated using 39 human cancer cell lines; averages of log IC50 values for conjugates 1 and 2 were -6.96 (110 nM) and -7.24 (57.5 nM), respectively. Conjugates 1 and 2 have potential as antitumor drugs capable of targeting telomere repeat sequence.
