170147-24-7Relevant articles and documents
Asymmetric Construction of 4 H-Pyrano[3,2-b]indoles via Cinchonine-Catalyzed 1,4-Addition of 2-Ylideneoxindole with Malononitrile
Zhou, Jin,Wang, Biao,He, Xiang-Hong,Liu, Li,Wu, Jun,Lu, Jing,Peng, Cheng,Rao, Chao-Long,Han, Bo
, p. 5450 - 5459 (2019)
A highly enantioselective [4 + 2] annulation of 2-ylideneoxindole with malononitrile has been accomplished by cinchonine catalysis under mild conditions. The corresponding enantiomerically enriched 4H-pyrano[3,2-b]indoles were generated in moderate to hig
A series of novel aryl-methanone derivatives as inhibitors of FMS-like tyrosine kinase 3 (FLT3) in FLT3-ITD-positive acute myeloid leukemia
Sellmer, Andreas,Pilsl, Bernadette,Beyer, Mandy,Pongratz, Herwig,Wirth, Lukas,Elz, Sigurd,Dove, Stefan,Henninger, Sven Julian,Spiekermann, Karsten,Polzer, Harald,Klaeger, Susan,Kuster, Bernhard,B?hmer, Frank D.,Fiebig, Heinz-Herbert,Kr?mer, Oliver H.,Mahboobi, Siavosh
, (2020/03/24)
Mutants of the FLT3 receptor tyrosine kinase (RTK) with duplications in the juxtamembrane domain (FLT3-ITD) act as drivers of acute myeloid leukemia (AML). Potent tyrosine kinase inhibitors (TKi) of FLT3-ITD entered clinical trials and showed a promising,
Design and synthesis of novel N-sulfonyl-2-indoles that behave as 5-HT6receptor ligands with significant selectivity for D3over D2receptors
Saavedra, Oscar M.,Rojas, Anne,Dupuis, Delphine,Gohier, Arnaud,Karila, Delphine,Ortuno, Jean-Claude,Mannoury la Cour, Clotilde,Brossard, Dominique,Millan, Mark J.,Hanessian, Stephen
, p. 38 - 52 (2016/12/22)
All clinically-used antipsychotics display similar affinity for both D2(D2R) and D3(D3R) receptors, and they likewise act as 5-HT2Areceptor antagonists. They provide therapeutic benefit for positive symptoms, but no marked
MAP4K4 (HGK) Inhibitors
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Paragraph 0254, (2016/08/10)
The invention provides mitogen-activated protein kinase kinase kinase kinase 4 (MAP4K4) inhibitors, and pharmaceutically acceptable salts, hydrides and stereoisomers thereof. The compounds are employed in pharmaceutical compositions, and methods of making and use, including treating a person in need thereof with an effective amount of the compound or composition, and detecting a resultant diminution of tumor cell growth, cancer or metastasis.
Synthesis of 3,5-bis(2-indolyl)pyridine and 3-[(2-indolyl)-5-phenyl]pyridine derivatives as CDK inhibitors and cytotoxic agents
Jacquemard, Ulrich,Dias, Nathalie,Lansiaux, Amelie,Bailly, Christian,Loge, Cedric,Robert, Jean-Michel,Lozach, Olivier,Meijer, Laurent,Merour, Jean-Yves,Routier, Sylvain
, p. 4932 - 4953 (2008/12/21)
We here report the synthesis and biological evaluation of new 3,5-bis(2-indolyl)pyridine and 3-[(2-indolyl)-5-phenyl]pyridine designed as potential CDK inhibitors. Indole, 5-hydroxyindole, and phenol derivatives were used to generate three substitutions o
CHEMICAL COMPOUNDS
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Page/Page column 77-78, (2008/06/13)
This invention relates to non-steroidal compounds that are modulators of androgen receptor, and also to the methods for the making and use of such compounds.
8-SULFONYL-L, 3, 4, 8-TETRAHYDR0-2H- [1, 4] OXAZEPINO [6, 7-E] INDOLE DERIVATIVES AND THEIR USE AS 5-HT6 RECEPTOR LIGANDS
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Page/Page column 70, (2008/12/05)
The present invention relates to compounds of the formula (I) wherein A, X and R1 to R9 are as described herein; to pharmaceutical compositions comprising the said compounds; to processes for their preparation; and to the use of the compounds as medicaments against 5-HT6 receptor-related disorders.
INDOLES AS 5-HT6 MODULATORS
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Page/Page column 133-134, (2008/06/13)
The present invention relates to novel compounds of formula (I) wherein m, n, R0, R1, R2, R3 and R4 are as described herein, to pharmaceutical compositions comprising the compounds, to processes for t
Inhibition of FLT3 and PDGFR tyrosine kinase activity by bis(benzo[b]furan-2-yl)methanones
Mahboobi, Siavosh,Uecker, Andrea,Cenac, Christophe,Sellmer, Andreas,Eichhorn, Emerich,Elz, Sigurd,Boehmer, Frank-D.,Dove, Stefan
, p. 2187 - 2197 (2008/02/01)
A series of bis(benzo[b]furan-2-yl)methanones was synthesized and tested for inhibition of FLT3 and PDGFR autophosphorylation. Mostly, C-5 substitution leads to PDGFR selectivity, which was strongest in the case of the 5,5′-dimethoxy derivative. The 5,5′-
Novel bis(1H-indol-2-yl)methanones as potent inhibitors of FLT3 and platelet-derived growth factor receptor tyrosine kinase
Mahboobi, Siavosh,Uecker, Andrea,Sellmer, Andreas,Cénac, Christophe,H?cher, Heymo,Pongratz, Herwig,Eichhorn, Emerich,Hufsky, Harald,Trümpler, Antje,Sicker, Marit,Heidel, Florian,Fischer, Thomas,Stocking, Carol,Elz, Sigurd,B?hmer, Frank-D.,Dove, Stefan
, p. 3101 - 3115 (2007/10/03)
FLT3 receptor tyrosine kinase is aberrantly active in many cases of acute myeloid leukemia (AML). Recently, bis(1H-indol-2-yl)methanones were found to inhibit FLT3 and PDGFR kinases. To optimize FLT3 activity and selectivity, 35 novel derivatives were synthesized and tested for inhibition of FLT3 and PDGFR autophosphorylation. The most potent FLT3 inhibitors 98 and 102 show IC 50 values of 0.06 and 0.04 μM, respectively, and 1 order of magnitude lower PDGFR inhibiting activity. The derivatives 76 and 82 are 20- to 40-fold PDGFR selective. Docking at the recent FLT3 structure suggests a bidentate binding mode with the backbone of Cys-694. Activity and selectivity can be related to interactions of one indole moiety with a Hydrophobic pocket including Phe-691, the only different binding site residue (PDGFR Thr-681). Compound 102 inhibited the proliferation of 32D cells expressing wildtype FLT3 or FLT3-ITD similarly as FLT3 autophosphorylation, and induced apoptosis in primary AML patient blasts.
