Within the last year
Within the past 3 years
1 - 10 of 63 articles
A variety of ω-substituted alkanoic acid (2-amino-phenyl)-amides were designed and synthesized. These compounds were shown to inhibit recombinant human histone deacetylases (HDACs) with IC 50 values in the low micromolar range and induce hyperacetylation of histones in whole cells. They induced...
D-optimal design and Projection to Latent Structures (PLS) analysis were used to optimize screening hit 5 ( B. subtilis AcpS IC 50 : 15 μM, B. subtilis MIC: >200 μM) into a series of 4 H -oxazol-5-one, small molecule, antibacterial, AcpS inhibitors. Specifically, 15 , 16 and 18 show μM or...
Several boronic acids were screened for their ability to bind to diols. 3-Methoxycarbonyl-5-nitrophenyl boronic acid bound to both a catechol dye as well as fructose with a comparable affinity to that of an ortho -methylamino substituted boronic acid. This work suggests a greater role for...
The synthesis and MMP inhibitory activity of a series of tetrahydroisoquinoline based sulfonamide hydroxamates are described. In nine MMPs tested, most of the compounds display potent inhibition activity except for MMP-7. Some subtle isozyme selectivity is observed by varying the substituents at...
Several semi-synthetic bis- and mono- O -alkyl nocathiacin derivatives were synthesized and evaluated for antibacterial activity. Mono- O -alkyl N -hydroxyindole analogues 3a – l were prepared by regioselective alkylation. Bis- O -alkyl nocathiacins 4a – f were obtained by treatment with base...
E7070 ( N -(3-chloro-7-indolyl)-1,4-benzenedisulfonamide) is an anticancer drug candidate under clinical development for the treatment of several types of cancers. We prove here that this compound also acts as a potent carbonic anhydrase (CA) inhibitor. Similarly to the clinically used drugs...
A new series of (4-(2-phenylethenesulfonylmethyl)phenyl)quinazolin-4-yl-amines was prepared and tested for its in vitro cytotoxic activity against a panel of 12 human cancer cell lines. Compounds 9 , 15 , 24 and 31 showed good in vitro activity and were further tested for their in vivo efficacy...
The addition of exogenous ent -cholesterol suppressed the antifungal activity of the amphotericin B when added to cultures of Candida albicans , but to a lesser extent than natural cholesterol. There were no detectable differences between added 2a or 2b on the antifungal activities of jaspamide...
Save this article to read later. You can see your Read Later on your DeepDyve homepage.
To save an article, log in first, or sign up for a DeepDyve account if you don't already have one.
Sign Up Log In
To subscribe to email alerts, please log in first, or sign up for a DeepDyve account if you don't already have one.
Read and print from thousands of top scholarly journals.
Sign up with Facebook
Sign up with Google
Already have an account? Log in
To get new article updates from a journal on your personalized homepage, please log in first, or sign up for a DeepDyve account if you don't already have one.