- Preparation of 5-substituted 2-carboxyindoles on solid support
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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.
- Tois, Jan,Franzén, Robert,Aitio, Olli,Huikko, Katri,Taskinen, Jyrki
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Read Online
- Oligomer modified diaromatic substituted compounds
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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
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- Indole-2-acetamide compound with anti-inflammatory effect, and application thereof in preparation of anti-inflammatory drugs
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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
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Paragraph 0051; 0053
(2016/10/27)
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- Synthesis and biological evaluation of antibody conjugates of phosphate prodrugs of cytotoxic DNA alkylators for the targeted treatment of cancer
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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
- Zhao, Robert Yongxin,Erickson, Hans K.,Leece, Barbara A.,Reid, Emily E.,Goldmacher, Victor S.,Lambert, John M.,Chari, Ravi V. J.
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experimental part
p. 766 - 782
(2012/03/11)
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- Structural influence of indole C5-N-substitutents on the cytotoxicity of seco-duocarmycin analogs
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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.
- Choi, Taeyoung,Ma, Eunsook
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experimental part
p. 357 - 367
(2012/05/04)
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- Synthesis and evaluation of a series of C5′-substituted duocarmycin SA analogs
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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.
- Robertson, William M.,Kastrinsky, David B.,Hwang, Inkyu,Boger, Dale L.
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body text
p. 2722 - 2725
(2011/07/06)
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- 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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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
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Page/Page column 37
(2009/10/22)
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- HETEROCYCLIC DERIVATIVES FOR MODULATION OF CALCIUM CHANNELS
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Heterocyclic derivatives act as Ca channel antagonists. The compositions are useful for treating or relieving Ca channel mediated conditions.
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Page/Page column 221
(2008/06/13)
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- AMINOMETHYL SUBSTITUTED BICYCLIC AROMATIC COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF THE DOPAMINE D3 RECEPTOR
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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
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Page/Page column 99
(2010/11/08)
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- Sequence-specific alkylation of double-strand human telomere repeat sequence by pyrrole-imidazole polyamides with indole linkers
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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.
- Sasaki, Shunta,Bando, Toshikazu,Minoshima, Masafumi,Shimizu, Tatsuhiko,Shinohara, Ken-Ichi,Takaoka, Toshiyasu,Sugiyama, Hiroshi
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p. 12162 - 12168
(2007/10/03)
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- Novel aromatic compounds possessing antifungal or antibacterial activity
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The present invention provides novel compounds possessing antibacterial, antifungal, antiviral, anticancer, and/or antiparasitic activities. Pharmaceutical compositions containing these compounds, methods of making and methods for using these compounds ar
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Page/Page column 60
(2010/02/06)
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- VIRAL POLYMERASE INHIBITORS
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An isomer, enantiomer, diastereoisomer or tautomer of a compound, represented by formula (I): wherein wherein A, B, R2, R3, L, M1, M2, M3, M4, Y1, Y0, Z and Sp are as defined in claim 1, or a salt thereof, as an inhibitor of HCV NS5B polymerase.
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- USE OF SUBSTITUTED 2,5-DIAMIDOINDOLES FOR THE TREATMENT OF UROLOGICAL DISEASES
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The present invention relates to the use of 2,5-diamidoindole derivatives for the preparation of medicaments for treating urological disorders in humans and/or animals.RCK 41-Foreign Countries
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- CC-1065 analog synthesis
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Improved synthesis of seco(?)CBI (5-hydroxy-3-amino-1-[S]-(chloromethyl)-1,2 -dihydro-3H-benz(e)indole): and improved syntheses therefrom of a wide variety of CC-1065 analogs that comprise a cyclopropabenzidole (CBI) alkylating moiety, and which are collectively DC1and its derivatives, for the synthesis of cell-targeted therapeutic agents.
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- Novel aromatic compounds and poly(oxyalkylene) containing aromatic compounds possessing antibacterial, antifungal or antitumor activity
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The present invention provides novel compounds possessing one or more of the following activities: antibacterial, antifungal and antitumor activity. The compounds are of Formula (I): Pharmaceutical compositions containing these compounds, methods of making and methods for using these compounds are also provided.
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- Novel compounds possessing antibacterial, antifungal or antitumor activity
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The present invention provides novel compounds possessing one or more of the following activities: antibacterial, antifungal and antitumor activity. The compounds are of Formula (I): Pharmaceutical compositions containing these compounds, methods of making and methods for using these compounds are also provided.
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- Cell binding agent conjugates of analogues and derivatives of CC-1065
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Novel cytotoxic agents comprising a cell binding agent chemically linked to one or more analogue or derivative of CC-1065 are described. The therapeutic use of the cytotoxic agents is also described. These cytotoxic agents have therapeutic use because the
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