- Full text PDF available (2)
Chk1 kinase is a critical component of the DNA damage response checkpoint especially in cancer cells and targeting Chk1 is a potential therapeutic opportunity for potentiating the anti-tumor activity of DNA damaging chemotherapy drugs. Fragment elaboration by structure guided design was utilized to identify and develop a novel series of Chk1 inhibitors… (More)
Computed Tomography (CT) is widely used for transportation security to screen baggage for potential threats. For example, many airports use X-ray CT to scan the checked baggage of airline passengers. The resulting reconstructions are then used for both automated and human detection of threats. Recently, there has been growing interest in the use of… (More)
We herein report the discovery of a novel class of antagonists of the human adenosine A2B receptor. This low molecular weight scaffold has been optimized to offer derivatives with potential utility for the alleviation of conditions associated with this receptor subtype, such as nociception, diabetes, asthma and COPD. Furthermore, preliminary pharmacokinetic… (More)
Libraries of nonpurified resorcinol amide derivatives were screened by surface plasmon resonance (SPR) to determine the binding dissociation constant (off-rate, kd) for compounds binding to the pyruvate dehydrogenase kinase (PDHK) enzyme. Parallel off-rate measurements against HSP90 and application of structure-based drug design enabled rapid hit to lead… (More)
Beta-allyloxy and beta-propargyloxy tert-butyl sulfoxides undergo tandem sulfoxide eliminination-intramolecular sulfenic acid addition reactions to produce 1,4-oxathiane S-oxides.
To lead positive change in the teaching practice of teams that service large numbers of diverse students from multiple degree programs provides many challenges. The primary aim of this study was to provide a clear framework on which to plan the process of change that can be utilized by academic departments sector wide. Barriers to change were reduced by… (More)
The explosive hexahydro-1,3,5-trinitro-s-triazine (CH2-N-NO2)3, commonly known as RDX, has been studied by 14N NQR and 1H NMR. NQR frequencies and relaxation times for the three ν+ and ν- lines of the ring 14N nuclei have been measured over the temperature range 230-330 K. The 1H NMR T1 dispersion has been measured for magnetic fields corresponding to the… (More)