cas 342405-28-1, 1-(PHENYLSULFONYL)-1H-INDOLE-2-CARBONYL CHLORIDE

Articles about 342405-28-1Total 4 be found

A convenient access to 1,3-disubstituted furo[3,4-b]indoles by acid ion-exchange resin-catalyzed furan formation
Efficient synthesis of furo[3,4-b]indoles starting from the corresponding indole is reported. The first route involves derivatization, protection, and deprotection steps, which stretch the syntheses. The second method provides a shorter and more efficient strategy to accessing the furoindole. The innovation starts with alkylation at C-2 of the indole presenting at the C-3 position a ketone-acetal, followed by the cycloaromatization catalyzed by polymeric ion-exchange resins. The second route represents a significant improvement over other methods previously described.
Basset, Joan,Romero, Manel,Serra, Tha?s,Pujol, M. Dolors
experimental part
p. 356 - 362
(2012/01/06)

Novel bis(1H-indol-2-yl)methanones as potent inhibitors of FLT3 and platelet-derived growth factor receptor tyrosine kinase
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.
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)

Novel indole derivatives, preparation thereof as medicinal products and pharmaceutical compositions, and especially as KDR inhibitors
The invention relates to compounds of formula (I): in which R1 represents pyrazolyl or indazolyl, R2 and R3 especially represent H, halogen, hydroxyl, nitro, cyano, R4, —OR4, —COR4, —OC(═O)R4, —C(═O)OR4, —C(═O)OH, —N(R5)C(═O)R4, —N(R5)C(═O)OR4, —S(O)nR4, —S(O)nOR4, —N(R5)SO2R4, —NY1Y2, —C(═O)NY1Y2, —N(R5)C(═O)NY1Y2, —S(O)nNY1Y2 and —OC(═O)NY1Y2, R4 especially represents alkyl, alkenyl, cycloalkyl, aryl, heteroaryl and heterocycloalkyl, R5 especially represents H, alkyl, alkenyl, cycloalkyl, heterocycloalkyl, aryl and heteroaryl, Y1 and Y2 especially represent H, alkyl, alkenyl, cycloalkyl, heterocycloalkyl, aryl, arylcarboxyl, heteroaryl and heteroarylcarboxy, which are optionally substituted, or Y1 and Y2 form with N an amino ring, n represents 0 to 2, all these radicals being optionally substituted, these products being in all the isomeric forms and the salts, as medicinal products, especially as KDR inhibitors.
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Page 22

(2008/06/13)

Bis(1H-2-indolyl)methanones as a novel class of inhibitors of the platelet-derived growth factor receptor kinase
The novel lead bis(1H-2-indolyl)methanone inhibits autophosphorylation of platelet-derived growth factor (PDGF) receptor tyrosine kinase in intact cells. Various substituents in the 5- or 6-position of one indole ring increase or preserve potency, whereas
Mahboobi, Siavosh,Teller, Steffen,Pongratz, Herwig,Hufsky, Harald,Sellmer, Andreas,Botzki, Alexander,Uecker, Andrea,Beckers, Thomas,Baasner, Silke,Sch?chtele, Christoph,überall, Florian,Kassack, Matthias U.,Dove, Stefan,B?hmer, Frank-D.
p. 1002 - 1018
(2007/10/03)