New Heterocyclic Combretastatin A-4 Analogs: Synthesis and Biological Activity of Styryl-2(3)-benzothiazolones.

Here, we describe the synthesis, characterization, and biological activities of a series of 26 new styryl-2(3H)-benzothiazolone analogs of combretastatin-A4 (CA-4). The cytotoxic activities of these compounds were tested in several cell lines (EA.hy926, A549, BEAS-2B, MDA-MB-231, HT-29, MCF-7, and MCF-10A), and the relations between structure and cytotoxicity are discussed.

Effects of increasing concentrations of fungicide Quadris on bacterial functional profiling in loamy sand soil.

A mesocosm experiment was conducted to assess the side effects of the fungicide Quadris on soil bacterial functioning. Quadris was applied to a loamy sand soil at increasing concentrations (0.0-35.

Aromatic F-C TROSY: a background-free approach to probe biomolecular structure, function, and dynamics.

Atomic-level information about the structure and dynamics of biomolecules is critical for an understanding of their function. Nuclear magnetic resonance (NMR) spectroscopy provides unique insights into the dynamic nature of biomolecules and their interactions, capturing transient conformers and their features. However, relaxation-induced line broadening and signal overlap make it challenging to apply NMR spectroscopy to large biological systems.

Combretastatin A-4 analogues with benzoxazolone scaffold: Synthesis, structure and biological activity.

In order to design and synthesize a new class of heterocyclic analogues of natural combretastatin A-4 and its synthetic derivative AVE8062, the benzoxazolone ring was selected as a scaffold for a bioisosteric replacement of the ring B of both molecules. A library of 28 cis- and trans-styrylbenzoxazolones was obtained by a modified Wittig reaction under Boden's conditions. Structures of the newly synthesized compounds bearing the 3,4,5-trimethoxy-, 3,4-dimethoxy-, 3,5-dimethoxy-, and 4-methoxystyryl fragment at position 4, 5, 6 or 7 of benzoxazolone core were determined on the basis of spectral and X ray data.

Ultrasound-assisted extraction of alantolactone and isoalantolactone from Inula helenium roots.

This work deals with ultrasound-assisted extraction (UAE) of alantolactone and isoalantolactone from the roots of Inula helenium L., a well-known medicinal plant. The effects of ethanol concentration, extraction time, temperature and number of extraction steps on the extraction yields of both sesquiterpene lactones were investigated.