In 2019,Bioorganic Chemistry included an article by Eldehna, Wagdy M.; Abo-Ashour, Mahmoud F.; Berrino, Emanuela; Vullo, Daniela; Ghabbour, Hazem A.; Al-Rashood, Sara T.; Hassan, Ghada S.; Alkahtani, Hamad M.; Almehizia, Abdulrahman A.; Alharbi, Amal; Abdel-Aziz, Hatem A.; Supuran, Claudiu T.. Name: N,N-Dimethylformamide Dimethyl Acetal. The article was titled 《SLC-0111 enaminone analogs, 3/4-(3-aryl-3-oxopropenyl) aminobenzenesulfonamides, as novel selective subnanomolar inhibitors of the tumor-associated carbonic anhydrase isoform IX》. The information in the text is summarized as follows:
SLC-0111, an ureido substituted benzenesulfonamide, is a selective carbonic anhydrase (CA, EC 4.2.1.1) IX inhibitor that is currently in Phase I/II clin. trials for the treatment of advanced hypoxic tumors complicated with metastases. Herein we report the synthesis of two series of 3/4-(3-aryl-3-oxopropenyl) aminobenzenesulfonamides 5a-i and 6a-j as SLC-0111 enaminone congeners. The prepared enaminones were in vitro investigated as inhibitors of the metalloenzyme carbonic anhydrase (CA, EC 4.2.1.1) isoforms hCA I, II, IV and IX, using a stopped-flow CO2 hydrase assay. All these isoforms were inhibited by the enaminones reported here in variable degrees. The target tumor-associated isoform hCA IX was undeniably the most affected one (KIs: 0.21-7.1 nM), with 6- to 21-fold enhanced activity than SLC-0111 (KI = 45 nM). All the prepared enaminones displayed interesting selectivity towards hCA IX over hCA I (SI: 32 – >35714), hCA II (SI: 2 – 1689) and hCA IV (SI: 11 – >45454). Of particular interest, bioisosteric replacement of Ph tail with the bulkier 2-naphthyl tail, sulfonamide 6h, achieved the higher II/IX selectivity herein reported with SI of 1689. After reading the article, we found that the author used N,N-Dimethylformamide Dimethyl Acetal(cas: 4637-24-5Name: N,N-Dimethylformamide Dimethyl Acetal)
N,N-Dimethylformamide Dimethyl Acetal(cas: 4637-24-5) belongs to anime. Nitrous acid converts secondary amines (aliphatic or aromatic) to N-nitroso compounds (nitrosamines): R2NH + HNO2 → R2N―NO. Some nitrosamines are potent cancer-inducing substances, and their possible formation is a serious consideration when nitrites, which are salts of nitrous acid, are present in foods or pharmaceutical preparations. Tertiary amines give rise to nitrosamines more slowly; an alkyl group is eliminated as an aldehyde or ketone, along with nitrous oxide, N2O.Name: N,N-Dimethylformamide Dimethyl Acetal
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