477844-46-5Relevant academic research and scientific papers
Improvements of C-H Radio-Iodination of N-Acylsulfonamides toward Implementation in Clinics
Babin, Victor,Benoist, Florian,Bouillon, Jean-Philippe,Cailly, Thomas,Dubost, Emmanuelle,Fabis, Frédéric,Hébert, Alexandra,Pigrée, Gilbert
, p. 4393 - 4400 (2019/11/21)
An improved protocol to perform C-H radio-iodination is described. These new conditions allow rapid and clean formation of radio-iodinated N-acylsulfonamides using [125 I]NIS and catalytic amounts of palladium acetate and para-toluenesulfonic a
Palladium-Mediated Site-Selective C-H Radio-iodination
Dubost, Emmanuelle,Babin, Victor,Benoist, Florian,Hébert, Alexandra,Barbey, Pierre,Chollet, Céline,Bouillon, Jean-Philippe,Manrique, Alain,Pieters, Grégory,Fabis, Frédéric,Cailly, Thomas
supporting information, p. 6302 - 6305 (2018/10/02)
The palladium-mediated C-H radio-iodination of arenes using sodium iodide as the primary isotopic source is reported and performed without chemical know-how in 30 min and applied to the synthesis of complex radio-iodinated compounds of biological interest.
An expeditious and convenient synthesis of acylsulfonamides utilizing polymer-supported reagents
Wang, Ying,Sarris, Kathy,Sauer, Daryl R.,Djuric, Stevan W.
, p. 5181 - 5184 (2008/02/08)
Acylsulfonamides can be rapidly and conveniently synthesized from a variety of carboxylic acids and sulfonamides utilizing the commercially available reagents, PS-DCC and DMAP under mild reaction conditions. DMAP can be efficiently scavenged by utilizatio
Acyl sulfonamide anti-proliferatives: Benzene substituent structure-activity relationships for a novel class of antitumor agents
Lobb, Karen L.,Hipskind, Philip A.,Aikins, James A.,Alvarez, Enrique,Cheung, Yiu-Yin,Considine, Eileen L.,De Dios, Alfonso,Durst, Gregory L.,Ferritto, Rafael,Grossman, Cora Sue,Giera, Deborah D.,Hollister, Beth A.,Huang, Zhongping,Iversen, Philip W.,Law, Kevin L.,Li, Tiechao,Lin, Ho-Shen,Lopez, Beatriz,Lopez, Jose E.,Martin Cabrejas, Luisa M.,McCann, Denis J.,Molero, Victoriano,Reilly, John E.,Richett, Michael E.,Shih, Chuan,Teicher, Beverly,Wikel, James H.,White, Wesley T.,Mader, Mary M.
, p. 5367 - 5380 (2007/10/03)
Two closely related diaryl acylsulfonamides were recently reported as potent antitumor agents against a broad spectrum of human tumor xenografts (colon, lung, breast, ovary, and prostate) in nude mice. Especially intriguing was their activity against colorectal cancer xenografts. In this paper, rapid parallel synthesis along with traditional medicinal chemistry techniques were used to quickly delineate the structure-activity relationships of the substitution patterns in both phenyl rings of the acylsufonamide anti-proliferative scaffold. Although the molecular target of the compounds remains unclear, we determined that the vascular endothelial growth factor-dependent human umbilical vein endothelial cells assay in combination with a soft agar disk diffusion assay allowed for optimization of potency in the series. The pharmacokinetic properties and in vivo activity in an HCT116 xenograft model are reported for representative compounds.
