Design, synthesis, and biological evaluation of dinuclear bismuth(III) complexes with Isoniazid-derived Schiff bases.

Four dinuclear bismuth(III) Schiff-base complexes bearing Schiff-base ligands have been synthesized and structurally characterized by single-crystal X-ray diffraction, elemental analysis, and spectral techniques (FT-IR, NMR and MS). The analytical data reveal the bismuth(III) complexes possess 1:1 metal-ligand ratios. In vitro biological studies have revealed that bismuth(III) complexes displayed much higher antibacterial and antitumor activities than their parent ligands, which involves two gram-negative (S. aureus, B. subtili) and two gram-positive (E. coli, P. aeruginosa) bacteria, and human gastric cancer SNU-16 cells. The power-time curves of S. pombe exposed to tested compounds were detected by bio-microcalorimetry. Some thermokinetic parameters (k, Pmax,tG and Qtotal) were derived based on the metabolic power-time curves, and their quantitative relationships with the concentrations (c) were further discussed.

Synthesis of nordihydroguaiaretic acid derivatives and their bioactivities on S. pombe and K562 cell lines.

Nordihydroguaiaretic acid (NDGA) and its synthetic analogues are potentially useful in treating diseases related to cancers, diabetes, viral and bacterial infections, and inflammation. In this paper, we report the optimal synthetic methods and the bioactivity study of terameprocol 2, NDGA derivative 3, and its cyclized analogue 4. The IC50 of these three compounds 2, 3 and 4 on the growth metabolism of Schizosacchromyces pombe and K562 cell lines were determined by microcalorimetry. The preliminary results showed that the compounds 2, 3 and 4 possessed good inhibition activities on S. pombe and K562 cell lines, and exhibited bidirectional biological effect and Hormesis effect. In particular, terameprocol 2 was found to possess the most potent inhibitory effect on K562 cell lines.

Synthesis and bioactive studies of complex 8-hydroxyquinolinato-bis-(salicylato) yttrium (III).

This paper reports the synthesis of a new bioactive complex, 8-hydroxyquinolinato-bis-(salicylato) yttrium (III) (HSAY), whose composition and structure were characterized by elemental analysis, IR spectra, thermogravimetric analysis, and X-ray diffraction. The power-time curves of the compounds HSAY, C(7)H(6)O(3), C(9)H(7)NO, and YCl(3)·6H(2)O on the growth metabolism of Schizosaccharomyces pombe (S. pombe) were determined at 32.00°C, respectively. The corresponding thermokinetics parameters, which include the microbial growth rate constant (κ), inhibition ratio (I), and half inhibition concentration (IC(50)), were also derived. The results showed that the generation time was 168.2 min, and all the compounds HSAY, C(7)H(6)O(3), C(9)H(7)NO, and YCl(3)·6H(2)O possessed good bioactivities on the growth metabolism of S. pombe, with the values of IC(50) being 0.055, 3.57, 0.057, and 1.35 mmol L(-1), respectively. The inhibition ability of these compounds above on the growth of the S. pombe has been observed to decrease in the order HSAY>C(9)H(7)NO>YCl(3)·6H(2)O>C(7)H(6)O(3).