R Thomas Swann

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The application of parallel synthesis to lead optimization programs in drug discovery has been an ongoing challenge since the first reports of library synthesis. A number of approaches to the application of parallel array synthesis to lead optimization have been attempted over the years, ranging from widespread deployment by (and support of) individual(More)
Arterial and venous blood gases were measured in the ovary of the Day-16-pregnant rat by a Van Slyke manometric technique. Concurrent observations of progestagen concentrations were also made to determine rates of hormone secretion. The oxygen consumption was 196.5 +/- 28.4 ml/min per kg ovarian tissue (mean +/- s.e.m., n = 8) which is amongst the highest(More)
Cytosolic phospholipase A2 (cPLA2) catalyzes the selective release of arachidonic acid from the sn-2 position of phospholipids and is believed to play a key cellular role in the generation of arachidonic acid. When assaying the human recombinant cPLA2 using membranes isolated from [3H]arachidonate-labeled U937 cells as substrate,(More)
Two stepwise procedures, developed for the introduction of the (E)-4-methyl-4-hexenoic acid side chain of mycophenolic acid, were used in the synthesis of monocyclic mycophenolic acid analogues 2a-i. The derivatives with a methyl group or hydrogen at C-4 and lacking the lactone moiety were much less cytotoxic than mycophenolic acid. The monocyclic analogues(More)
A novel protocol which employs commercially available, standard tools and hardware has been developed. This protocol allows for cleavage and collection of IRORI Microkan products in 96 well plate format. Typically, 640 compounds can be cleaved in a 4 hour time period using approximately 3 square feet of space. This protocol has been used successfully for(More)
Rats at Day 16 of pregnancy were infused, via the parametrial artery, with radioactively labelled acetate or cholesterol. All of the venous effluent was collected and examined for radioactive progesterone and related compounds. Labelled progesterone was found in the venous effluent within 15 and 30 min of the start of cholesterol and acetate infusions,(More)
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