The Score Card Approach: A First Step Toward an Evidence-based Differentiation Assessment for Tablets.

Background: The differentiation of tablets by their physical appearance is a contributing factor to the safe use of medications. In this study, a "score card" was developed to assess how well one tablet is differentiated from another tablet on the basis of the physical attributes of color, size, and shape.

Methods: The score card was derived from a "2-out-of-5" difference test, in which participants were presented with groups of 5 tablets with varying color, size, and shape, and were asked to identify the 2 tablets that were different from the other 3 tablets.

Cell cycle-dependent cytotoxicity and mitotic spindle checkpoint dependency of investigational and approved antimitotic agents.

The mitotic spindle checkpoint (SPC) is a highly regulated mechanism in eukaryotic cells that ensures the even distribution of the duplicated genome between daughter cells. Malfunction of the SPC or deregulated expression of SPC regulatory proteins is frequently associated with a poor response to chemotherapeutic agents. We investigated various approved and investigational mitosis-specific agents, including spindle poisons, an Eg5 kinesin inhibitor, inhibitors of polo-like kinase 1 (Plk1) or Aurora-B kinase, a benzamide class HDAC inhibitor and compounds identified in a chemical genetics screen for their cell cycle-dependent cytotoxicities and for their activities toward SPC deficient (HT29, Caco-2, T47D) and SPC proficient human cell lines (A2780, HCT116, SW480).

A nucleophile-catalyzed cycloisomerization permits a concise synthesis of (+)-harziphilone.

Substantial structural transformations of much use in complex chemical synthesis can be achieved by channeling the reactivity of highly unsaturated molecules. This report describes the direct conversion of an acyclic polyunsaturated diketone to the HIV-1 Rev/Rev-responsive element inhibitor harziphilone under mild reaction conditions.

A variable concept for the preparation of branched glycosyl phosphatidyl inositol anchors.

A variable concept for the synthesis of branched glycosyl phosphatidyl inositol (GPI) anchors was established. Its efficiency could be shown by the successful synthesis of the GPI anchor of rat brain Thy-1 and of the scrapie prion protein both in the water soluble 1c and lipidated form 1a. Retrosynthesis led to building blocks 2-6 of which 5 could be further disconnected to building blocks 7-9.