Krymov, Stepan K. published the artcileSynthesis, biological evaluation, and in silico studies of potential activators of apoptosis and carbonic anhydrase inhibitors on isatin-5-sulfonamide scaffold, Product Details of C8H6ClF3, the publication is European Journal of Medicinal Chemistry (2022), 113997, database is CAplus and MEDLINE.
Carbonic anhydrase IX is a promising target for the search for new antitumor compounds with improved properties. Using the mol. hybridization approach, on the basis of structures of a selective carbonic anhydrase IX inhibitor 3 and an activator of apoptosis 2 (1), a series of 1-substituted isatin-5-sulfonamides I [R = benzyl, 2-fluorobenzyl, 3-fluorobenzyl, etc.] were designed and synthesized. The study of the inhibitory activity of isatin-5-sulfonamides showed the ability to inhibit I, II, IX, XII isoforms at nano- and micromolar concentrations Docking of compounds 1-(3,5-Difluorobenzyl)-2,3-dioxoindoline-5-sulfonamide and 1-(2,4-Dichlorobenzyl)-2,3-dioxoindoline-5-sulfonamide into the active site of II and IX carbonic anhydrase isoforms showed the coordination of sulfonamidate anions with zinc cations, as well as a number of addnl. hydrophobic interactions. The trifluoromethylthio derivative2,3-Dioxo-1-(4-((trifluoromethyl)thio)benzyl)indoline-5-sulfonamide suppressed the growth of tumor cells at low micromolar concentrations, maintaining activity on resistant lines and under hypoxic conditions. Immunoblotting of MCF7 cells treated with the 2,3-Dioxo-1-(4-((trifluoromethyl)thio)benzyl)indoline-5-sulfonamide revealed its antiestrogenic activity and ability to activate apoptosis in tumor cells.
European Journal of Medicinal Chemistry published new progress about 939-99-1. 939-99-1 belongs to chlorides-buliding-blocks, auxiliary class Fluoride,Chloride,Benzyl chloride,Benzene, name is 1-(Chloromethyl)-4-(trifluoromethyl)benzene, and the molecular formula is C8H6ClF3, Product Details of C8H6ClF3.
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