Observations on salicyl hydroxamic acid, an experimental trypanocide

1981 ◽  
Vol 37 (12) ◽  
pp. 1290-1291 ◽  
Author(s):  
A. J. Barnicoat ◽  
W. G. van't Hoff ◽  
P. J. Morrison ◽  
H. J. Rogers
JOM ◽  
2018 ◽  
Vol 70 (12) ◽  
pp. 2813-2818 ◽  
Author(s):  
Wei Yao ◽  
Maolin Li ◽  
Rui Cui ◽  
Xingke Jiang ◽  
Hongqiang Jiang ◽  
...  

2016 ◽  
Vol 623 ◽  
pp. 43-49 ◽  
Author(s):  
Gui-bin Lu ◽  
Cai-xing Zhang ◽  
Wang-hua Chen ◽  
Li-ping Chen ◽  
Yi-shan Zhou

Genetics ◽  
1979 ◽  
Vol 93 (3) ◽  
pp. 539-555
Author(s):  
Thad H Pittenger ◽  
David J West

ABSTRACT Filtration-enrichment and inositol-less death methods of mutant isolation, coupled with a screen for cyanide-insensitive respiration, proved to be highly efficient methods for isolating temperature-sensitive (ts) nuclear Neurospora mutants having defective respiration. Eighteen different ts respiratory mutants have been isolated. Most of them are pleiotropic and defective in one or more of the following phenotypes: cytochrome aa3, b, and c (individual or multiple defects); oligomycin inhibition of ATPase activity; respiration and its inhibition by KCN and salicyl hydroxamic acid; and growth rates in liquid and solid media at 25° and 38°. Among these mutants are the first cytochrome c mutant of Neurospora and an extranuclear ts ATPase mutant. An added bonus was the fact that aver half of the mutants were affected either in ribosome assembly or in protein synthesis in the mitochondrion. We have yet to find any mutants completely lacking activities associated with the respiratory chain. However, the wide spectrum of mutants isolated here, along with those currently available, constitutes a considerable resource for investigating respiration in obligate aerobes.


2013 ◽  
Vol 52 (1-2) ◽  
pp. 139-147 ◽  
Author(s):  
Janusz Czapski

Latent form of mushroom catechol oxidase was activated by O,1% sodium dodecyl sulfate (SDS). Catalytic power of the latent form, calculated from the kinetic parameters was 1,8 times higher than that of active one. Salicyl hydroxamic acid (SHAM) appeared as a powerful inhibitor for both active and latent forms of catechol oxidase. However, in the range of 150-250 μM SHAM the inhibitory effect for active catechol oxidase was significantly higher than that for the latent one. Non-competitive and irreversible characteristics of inhibition of latent and active catechol oxidase was calculated from kinetic data. Electrophoretic analysis followed by scanning of the gels was used. The spots' absorbance was determined from a computer image of the isoenzyme band patterns. It allowed us to estimate gels quantitatively. Presence of one additional clearly defined slow moving isoform of SDS-activated catechol oxidase, differed in the respect of 3 bands for the active and 4 bands for the total.


2019 ◽  
Vol 19 (7) ◽  
pp. 916-934 ◽  
Author(s):  
Appavoo Umamaheswari ◽  
Ayarivan Puratchikody ◽  
Natarajan Hari

Background:The available treatment option for any type of cancer including CTCL is chemotherapy and radiation therapy which indiscriminately persuade on the normal cells. One way out for selective destruction of CTCL cells without damaging normal cells is the use of histone deacetylase inhibitors (HDACi). Despite promising results in the treatment of CTCL, these HDACi have shown a broadband inhibition profile, moderately selective for one HDAC class but not for a particular isotype. The prevalence of drug-induced side effects leaves open a narrow window of speculation that the decreased therapeutic efficacy and observed side effects may be most likely due to non specific HDAC isoform inhibition. The aim of this paper is to synthesis and evaluates HDAC8 isoform specific inhibitors.Methods:Based on the preliminary report on the design and in silico studies of 52 hydroxamic acid derivatives bearing multi-substituent heteroaromatic rings with chiral amine linker, five compounds were shortlisted and synthesized by microwave assisted approach and high yielding synthetic protocol. A series of in vitro assays in addition to HDAC8 inhibitory activity was used to evaluate the synthesised compounds.Results:Inhibitors 1e, 2e, 3e, 4e and 5e exerted the anti-proliferative activities against CTCL cell lines at 20- 100 µM concentrations. Both the pyrimidine- and pyridine-based probes exhibited μM inhibitory activity against HDAC8. The pyrimidine-based probe 1e displayed remarkable HDAC8 selectivity superior to that of the standard drug, SAHA with an IC50 at 0.1µM.Conclusion:Our study demonstrated that simple modifications at different portions of pharmacophore in the hydroxamic acid analogues are effective for improving both HDAC8 inhibitory activity and isoform selectivity. Potent and highly isoform-selective HDAC8 inhibitors were identified. These findings would be expedient for further development of HDAC8-selective inhibitors.


Sign in / Sign up

Export Citation Format

Share Document