Unknown

Dataset Information

0

Synthesis, Biological Evaluation and Molecular Modeling of Substituted Indeno[1,2-b]indoles as Inhibitors of Human Protein Kinase CK2.

ABSTRACT: Due to their system of annulated 6-5-5-6-membered rings, indenoindoles have sparked great interest for the design of ATP-competitive inhibitors of human CK2. In the present study, we prepared twenty-one indeno[1,2-b]indole derivatives, all of which were tested in vitro on human CK2. The indenoindolones 5a and 5b inhibited human CK2 with an IC50 of 0.17 and 0.61 µM, respectively. The indeno[1,2-b]indoloquinone 7a also showed inhibitory activity on CK2 at a submicromolar range (IC50 = 0.43 µM). Additionally, a large number of indenoindole derivatives was evaluated for their cytotoxic activities against the cell lines 3T3, WI-38, HEK293T and MEF.

SUBMITTER: Alchab F 

PROVIDER: S-EPMC4491662 | biostudies-literature | 2015 Jun

REPOSITORIES: biostudies-literature

Json Xml
altmetric image

Publications

Synthesis, Biological Evaluation and Molecular Modeling of Substituted Indeno[1,2-b]indoles as Inhibitors of Human Protein Kinase CK2.

Alchab Faten F   Ettouati Laurent L   Bouaziz Zouhair Z   Bollacke Andre A   Delcros Jean-Guy JG   Gertzen Christoph G W CG   Gohlke Holger H   Pinaud Noël N   Marchivie Mathieu M   Guillon Jean J   Fenet Bernard B   Jose Joachim J   Borgne Marc Le ML  

Pharmaceuticals (Basel, Switzerland) 20150608 2

Due to their system of annulated 6-5-5-6-membered rings, indenoindoles have sparked great interest for the design of ATP-competitive inhibitors of human CK2. In the present study, we prepared twenty-one indeno[1,2-b]indole derivatives, all of which were tested in vitro on human CK2. The indenoindolones 5a and 5b inhibited human CK2 with an IC50 of 0.17 and 0.61 µM, respectively. The indeno[1,2-b]indoloquinone 7a also showed inhibitory activity on CK2 at a submicromolar range (IC50 = 0.43 µM). Ad  ...[more]

Similar Datasets

Unknown Development of Pharmacophore Model for Indeno[1,2-b]indoles as Human Protein Kinase CK2 Inhibitors and Database Mining.
| S-EPMC5374412 | biostudies-literature
Unknown Synthesis, biological evaluation, and molecular modeling of 11H-indeno[1,2-b]quinoxalin-11-one derivatives and tryptanthrin-6-oxime as c-Jun N-terminal kinase inhibitors.
| S-EPMC6261293 | biostudies-literature
Unknown Broad-Spectrum Anticancer Activity and Pharmacokinetic Properties of a Prenyloxy-Substituted Indeno[1,2-b]indole Derivative, Discovered as CK2 Inhibitor.
| S-EPMC8226678 | biostudies-literature
Unknown Unexpected Binding Mode of a Potent Indeno[1,2-b]indole-Type Inhibitor of Protein Kinase CK2 Revealed by Complex Structures with the Catalytic Subunit CK2? and Its Paralog CK2?'.
| S-EPMC5748653 | biostudies-literature
Unknown Mechanistic basis of breast cancer resistance protein inhibition by new indeno[1,2-b]indoles.
| S-EPMC7815716 | biostudies-literature
Unknown Synthesis of Some Spiro Indeno[1,2-b]pyrido[2,3-d]Pyrimidine-5,3'-Indolines as New Urease Inhibitors.
| S-EPMC5242352 | biostudies-literature
Unknown Novel c-Jun N-Terminal Kinase (JNK) Inhibitors with an 11H-Indeno[1,2-b]quinoxalin-11-one Scaffold.
| S-EPMC8464905 | biostudies-literature
Unknown [b]-Annulated Halogen-Substituted Indoles as Potential DYRK1A Inhibitors.
| S-EPMC6891749 | biostudies-literature
Unknown Synthesis, biological evaluation, and physicochemical property assessment of 4-substituted 2-phenylaminoquinazolines as Mer tyrosine kinase inhibitors.
| S-EPMC4920374 | biostudies-literature
Unknown A Simple and Efficient Synthesis of Highly Substituted Indeno[1,2-<i>b</i>]pyrrole and Acenaphtho[1,2-<i>b</i>]pyrrole Derivatives by Tandem Three-Component Reactions.
| S-EPMC6278260 | biostudies-literature