Anti-Mycobacterial N-(2-Arylethyl)quinolin-3-amines Inspired by Marine Sponge-Derived Alkaloid.

The synthesis and evaluation of simplified analogs of marine sponge-derived alkaloid 3-(phenethylamino)demethyl(oxy)aaptamine were performed to develop novel anti-mycobacterial substances. Ring truncation of the tricyclic benzo[de][1,6]-naphthyridine skeleton effectively weakened the cytotoxicity of the natural product, and the resulting AC-ring analog exhibited good anti-mycobacterial activity. A structure-activity relationship (SAR) study, synthesizing and evaluating some analogs, demonstrated the specificity and importance of the N-(2-arylethyl)quinolin-3-amine skeleton as a promising scaffold for anti-mycobacterial lead compounds.

In vivo measurement of vertebral endplate surface area along the whole-spine.

Accurate determination of vertebral endplate surface area and diameters plays an important role in surgical procedures, spinal implant design and sizing. The objective of this study was to contribute with baseline information on the endplate geometrical parameters using subject-based 3D whole-spine computed tomography (CT) models based on myelogram CT images taken of 49 patients with spinal disorders. Superior and inferior bony endplate mesh-models were created from said 3D CT models and endplate geometrical parameters including total polygon-mesh areas, projected areas and antero posterior and transverse diameters of each endplate were measured. The position of each endplate was determined by the cumulative distance along the spinal column with respect to C2. Endplate area and diameters were analyzed by gender, spinal level, age and correlation with spinal position. Males had larger endplates than females at all levels (p < 0.05) but S1. While endplate areas and transverse diameters increased with age at C3-L5 in females, these increases were not consistent through the whole-spine and even decreases with age were found at T1-T3 in males. There was a strong linear correlation between endplate area and spinal position in males and females with correlation coefficient values of r = 0.938 and r = 0.911, respectively. However, multiple comparisons of the geometrical parameters through the whole-spine revealed localized reduction of the anteroposterior or transverse diameters at T4 and L5-S1 levels. These regional and age-related changes in endplate dimensions should be taken into account for safe interventional treatments at these sites. © 2016 Orthopaedic Research Society. Published by Wiley Periodicals, Inc. J Orthop Res 34:1418-1430, 2016.

Synthesis and structure-activity relationship studies of furan-ring fused chalcones as antiproliferative agents.

As part of our continuing investigation of flavonoid derivatives as potential anticancer substances, the synthesis of 25 cinnamoyl derivatives of benzofuran as furan-fused chalcones was carried-out and these compounds were further evaluated for their antiproliferative activity towards HL60 promyelocytic leukemia cells. In comparison with 2',4'-dihydroxychalcone, attachment of a furan moiety on the A-ring enhanced activity by more than twofold. Benzofurans may be useful in the design of biologically active flavonoids.