Journal ArticleDOI
Design, Synthesis, and in vitro Evaluation of Tubulin-Targeting Dibenzothiazines with Antiproliferative Activity as a Novel Heterocycle Building Block.
Walter D. Guerra,Daniel Lucena-Agell,Rafael Hortigüela,Roberto A. Rossi,J. Fernando Díaz,José M. Padrón,Silvia M. Barolo +6 more
TLDR
In this article, a series of free NH and N-substituted dibenzonthiazines with potential anti-tumor activity from N-aryl-benzenesulfonamides were presented.Abstract:
We prepared a series of free NH and N-substituted dibenzonthiazines with potential anti-tumor activity from N-aryl-benzenesulfonamides. A biological test of synthesized compounds (59 samples) was performed in vitro measuring their antiproliferative activity against a panel of six human solid tumor cell lines and its tubulin inhibitory activity. We identified 6-(phenylsulfonyl)-6H-dibenzo[c,e][1,2]thiazine 5,5-dioxide and 6-tosyl-6H-dibenzo[c,e][1,2]thiazine 5,5-dioxide as the best compounds with promising values of activity (overall range of 2-5.4 μM). Herein, we report the dibenzothiazine core as a novel building block with antiproliferative activity, targeting tubulin dynamics.read more
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Sulfoxylate Anion Radical-Induced Aryl Radical Generation and Intramolecular Arylation for the Synthesis of Biarylsultams.
Joydev K. Laha,P. Gupta +1 more
TL;DR: The sulfoxylate anion radical (SO2-•), generated in situ from the reagents rongalite or sodium dithionite (Na2S2O4), was found to be the key single electron transfer agent forming aryl radicals from aRYl halides, which upon intramolecular arylation gives biarylsultams with good to excellent yields.
Journal ArticleDOI
Integrated nickel/polymer dual catalytic system for visible-light-driven sulfonamidation between aryl halides and aryl sulfonamides
TL;DR: In this article , an integrated dual catalytic system of porous carbon nitride nanosheet with nitrogen vacancies (N V -P-C 3 N 4 ) was constructed by a defect and morphology regulation strategy toward visible-light-driven sulfonamidation between aryl halides and alkyl amines.
Journal ArticleDOI
Nickel-Catalyzed Denitrogenative Cyclization of 1,2,3,4-Benzothiatriazin-1,1(2H)-dioxides with Arynes To Synthesize Biaryl Sultams.
TL;DR: In this paper , the authors reported the nickel-catalyzed denitrogenative cyclization reaction of 1,2,3,4-benzothiatriazine-1,1-dioxides with arynes to generate the polysubstituted biaryl sultams with tolerance of a wide diversity of substituents on every subunit.
Journal ArticleDOI
Intramolecular Arylation of 2‐Bromobenzenesulfonamides Using DMSO/HCOONa·2H2O System: An Access To Dibenzosultams
TL;DR: In this paper , six or seven-membered dibenzosultams were synthesized upon treatment of N-aryl- or N-benzyl-2-halobenzenesulfonamides with HCOONa·2H2O in DMSO without using additional measures and additives, such as light irradiation, electrochemical apparatus, transition metals, and oxidants.
References
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