An ebselen like catalyst with enhanced GPx activity via a selenol intermediate

Abstract

The reaction of KSeO(t)Bu with 2-iodo-arylbenzamides gave benzamide ring-substituted, quinine-derived isoselenazolones 1b–1d. The reaction of PhSH with ortho-methyl-substituted isoselenazolone 1b gave selenol 3b, which is oxidized by H2O2 to regenerate 1b. Isoselenazolone 1b shows a high rate (0.33 × 103 μM min(−1)) of oxidation of PhSH with H2O2, which is ∼103-fold more active than ebselen (1a) and ≥30-fold more active than the other isoselenazolones of this study. Compound 1b shows less inhibition of the growth of yeast cells than 1a.

Diastereoselective desymmetrization of diarylphosphinous acid-borane amides under Birch reduction

“…21 Data are in accordance with those reported in the literature. 23 Data are in accordance with those reported in the literature. This compound was prepared according to the literature procedure.…”

Assessment of the Biological Pathways Targeted by Isocyanate Using N-Succinimidyl N-Methylcarbamate in Budding Yeast Saccharomyces cerevisiae

“…To investigate the biological effect of NSNM on the growth of yeast cells, growth assay was carried out by spot testing (as described earlier [14], [15]) using serial dilutions of mid-log phase cultures of wild-type and different mutant strains listed in Table S1. 3 μl of each undiluted and 10-fold serially diluted culture were spotted onto solid SCA plates containing vehicle DMSO or different concentrations of NSNM (100 and 200 μM).…”

Anti‐cancer drug KP1019 modulates epigenetics and induces DNA damage response in Saccharomyces cerevisiae

“…Therefore, we employed various yeast histone tail mutants to investigate the effect of KP1019. Removal of N-terminal tail of H2A (1)(2)(3)(4)(5)(6)(7)(8)(9)(10)(11)(12)(13)(14)(15)(16)(17)(18)(19)(20) or H3(1-30) leads to hypersensitivity to KP1019 (Fig. 3A) suggesting that these regions of histone tails are crucial for providing resistance to this drug.…”

“…To investigate the biological effect of KP1019 on the growth of yeast cells, growth assay was carried out through spot tests as described earlier [19,20] was measured at regular intervals for 6 h. Clonogenic assay was carried as described earlier [15]. Equal number of mid-log phase cells from untreated (DMSO) and KP1019 treated cultures (3 h) were spread on SCA plates.…”