A series of N-mustards, which was conjugated to mono- or bis-naphthalimides with a flexible amine link, were synthesized and evaluated for cytotoxicity against five cancer cell lines (HCT-116, PC-3, U87 MG, Hep G2 and SK-OV-3). Several compounds displayed better activities than the control compound amonafide. Further evaluations by fluorescence spectroscopy studies and DNA-interstrand cross-lin...

Novel antioxidants have been synthesized and characterized by their chemical properties as antioxidants with high superoxide scavenging activity. (2R,3R)-diphenylethylenediamine is a spacer in antioxidants, and we synthesized targets 11a and 11b by conjugation with o-hydroquinone and p-hydroquinone at the two N-termini, respectively. Superoxide scavenging activities of the plant flavonoid-like ...

Disproportionation reactions of chlorosilane compounds in the presence boron trichloride yield compound H[B(SiCl3)4]. Spectroscopic analyses yellow-whitish solid with IR-, Raman-, and NMR-spectroscopy (29Si, 11B) show a highly symmetric anion containing boron, which is fourfold coordinated silicon. Due to high symmetry 1J(11B,29Si) even 1J (10B, 29Si) couplings can be observed NMR spectra disso...

11b-Hydroxysteroid dehydrogenase type 1 (11b-HSD1) is considered a potential therapeutic target in the treatment of type 2 diabetes mellitus. In this study, we investigated the pharmacological properties of HIS-388 (N-[(1R,2s,3S,5s,7s)-5-hydroxyadamantan-2yl]-3-(pyridin-2-yl) isoxazole-4-carboxamide), a newly synthesized 11b-HSD1 inhibitor, using several mouse models. In cortisone pellet–implan...

A substantial amount of evidence has proposed an important role for Cyclooxygenase-2 (COX-2) enzyme in brain diseases and affiliate disorders. The purpose of this research was studying the effects of COX-2 selective inhibition on haloperidol-induced catatonia in an animal model of drug overdose and Parkinson’s disease (PD). In this study, the effect of acute and Sub-chronic oral administration ...

Recent trials show salicylates improve glycemic control in type 2 diabetes, but the mechanism is poorly understood. Expression of the glucocorticoid-generating enzyme 11b-hydroxysteroid dehydrogenase type 1 (11b-HSD1) in adipose tissue is increased in vitro by proinflammatory cytokines and upregulated in obesity. 11b-HSD1 inhibition enhances insulin sensitivity. We hypothesized that salicylates...

The title compound, C(20)H(30)O(2), {systematic name: (4aR,6aS,7R,11aS,11bR)-4,4,7,11b-tetra-methyl-1,2,3,4,4a,5,6,6a,7,11,11a,11b-dodeca-hydro-phenanthro[3,2-b]furan-4a-ol}, is a cas-sane furan-oditerpene which was isolated from the roots of Caesalpinia pulcherrima. The absolute configurations at positions 4a, 6a, 7, 11a and 11b are R, S, R, S and R, respectively. The mol-ecule has four-fused ...

The title compound, C(27)H(34)O(5) {systematic name: (4aR,5R,6R,6aS,7R,11aS,11bR)-4a,6-dihy-droxy-4,4,7,11b-tetra-methyl-1,2,3,4,4a,5,6,6a,7,11,11a,11b-dodeca-hydro-phenanthro[3,2-b]furan-5-yl benzoate}, is a cassane furan-oditerpene, which was isolated from the roots of Caesalpinia pulcherrima. The three cyclo-hexane rings are trans fused: two of these are in chair conformations with the third...

Glucocorticoids (GCs) act via intracellular mineralocorticoid (MR) and glucocorticoid receptors (GR). However, it has recently been recognized that GC access to receptors is determined by the presence of tissue-specific 11b-hydroxysteroid dehydrogenases (11b-HSDs) that catalyze the interconversion of active corticosterone and inert 11-dehydrocorticosterone. 11b-HSD type 1 (11b-HSD1) is a bidire...