Synthesis and anticancer activity of new benzensulfonamides incorporating s-triazines as cyclic linkers for inhibition of carbonic anhydrase IX.

ABSTRACT: Limited presence of hCA IX in normal physiological tissues and their overexpression only in solid hypoxic tumors made this isoform excellent possible target for developing new anticancer agents. We reported designing and synthesis of two novel series of benzenesulfonamides derivatives as hCA IX inhibitors bearing rigid cyclic linkers (1,3,5-dihydrotriazine in series A and 1,3,5-triazine in series B) in replace of traditional linear linkers. Also, novel cyanoethenyl spacer was assembled next to the 1,3,5-triazine linker in series B. Target compounds of series (A) and (B) were screened against four hCA isoforms. Human CA IX efficiently inhibited in series (A) by compound 5a (K_I = 134.8 nM). Meanwhile, in series (B) the most active inhibitor was 12i (K_I = 38.8 nM). US-NC

SUBMITTER: Zain-Alabdeen AI 

PROVIDER: S-EPMC9537541 | biostudies-literature | 2022 Oct

REPOSITORIES: biostudies-literature