Discovery research samples

The isolation of the benzolactone enamide salicylihalamide A 17101 (Scheme 6.1 Part 2) was guided by the NCI s Drug Discovery Research and Development, Developmental Therapeutics Program screen for differential cytotoxicity, which showed that the Australian sample of Haliclona possessed a unique 60 cell line profile. Nanomolar potency was evident in the melanoma cell lines (GI50 = 7 nM) and a COMPARE analysis of the 60 cell line data indicated vascular ATPase (V-ATPase) activity potential. Further study of this structure class determined that salicylihalamide A is equipotent to the V-ATPase standards bafilomycin A and concanamycin A,273 but unlike these standards, selectively inhibits mammalian V-ATPases. 

Figure 6 shows a commercially available robotic system that can automatically dispense precise quantities of a powder into a rack of vials, which is one of the time-consuming steps involved in reactor loa g. However, this particular system is designed to dispense a single powder into multiple vials as typically encountered in pharmaceutical discovery research. In catalyst discovery, the robotic design would require modification to handle multiple powders that would be created in a synthesis robot. A key requirement would be to minimize cross sample contamination. 

Phenyl-ethyl alcohol, or benzyl carbinol, has been known for many years, but its powerful rose odour has been entirely overlooked, its discovery having been made by an ordinary research chemist and not a perfumery expert. Its preparation was described in the Berichte (9, 373) in 1876, but the product there noted was evidently impure, as its boiling-point is recorded as 212°. Commercial specimens vary greatly in both their odour and their keeping properties, some samples deteriorating in odour very rapidly. It is, therefore, very important to -obtain it in a state of the highest purity. It has the following characters —... 

Much research on the Hishikari deposits has been carried out since the discovery of gold veins in 1981. Urashima and Izawa (1983) reported fluid inclusion studies using core samples. Abe et al. (1986) made a detailed description of the veins. The regional geology of this district is described in MMAJ and SMM (1987) and Urashima et al. (1987). 

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