Thiophosphorylation of Pharmacophoric Phenols,Diols, and Triols

Abstract

Novel organyldithiophosphonic and bis(aryldithiophosphonic) acids were obtained by the reaction of 2,4-diorganyl 1,3,2,4-dithiadiphosphetane-2,4-disulfides with paracetamol, 4-(1H-pyrrol-1-yl)phenol, ethambutol dihydrochloride, vitamin B₆, and its acetonide derivatives.     

Phosphorylation of polyesterpolyoles Boltorn-H20 and -H40 with pyrocatechol chlorophosphite

Russian Journal of Organic Chemistry -     

Tumor suppressor Fhit protein interacts with protoporphyrin IX in vitro and enhances the response of HeLa cells to photodynamic therapy

Fhit, the product of tumor suppressor fragile histidine triad (FHIT) gene, exhibits antitumor activity of still largely unknown cellular background. However, it is believed that Fhit-Ap(3)A or Fhit-AMP complex might act as a second class messenger in cellular signal transduction pathway involved in cell proliferation and apoptosis. We demonstrate here for the first time that the photosensitizer, protoporphyrin IX (which is a natural precursor of heme) binds to Fhit protein and its mutants in the active site in vitro. Furthermore, PpIX inhibits the enzymatic activity of Fhit. Simultaneously, PpIX shows lower binding capacity to mutant Fhit-H96N of highly reduced hydrolase activity. In cell-based assay PpIX induced HeLa cell death in Fhit and Fhit-H96N-dependent manner which was measured by means of MTT assay. Moreover, HeLa cells stably expressing Fhit or mutant Fhit-H96N were more susceptible to protoporphyrin IX-mediated photodynamic therapy (2J/cm(2)) than parental cells.     

Plasmon-enhanced luminescence of CdSe quantum dots on the porous silicon with silver nanoparticles

Russian Chemical Bulletin -     

Evaluation of Wound-Healing and Antioxidant Effects of Marantodes pumilum (Blume) Kuntze in an Excision Wound Model

Marantodes pumilum (MP) is a great source of herbal medicine used traditionally by both men and women for various purposes. MP may have potential wound-healing effects due to its diverse biological properties. An extensive study was conducted in a normal male rat model for determining the effects of MP var. pumila (MPvp) and var. alata (MPva) on the wound healing process. Here, 126 male Sprague-Dawley rats were divided randomly into seven groups as follows: sham-operated (SH), vehicle dressing (VD), flavine dressing (FD), MPvp leaves (PL), MPvp roots (PR), MPva leaves (AL), and MPva roots (AR). The parameters studied were the percentage of wound contraction, histomorphology study by hematoxylin and eosin (H&E), Masson–Goldner trichrome (MGT), and immunohistochemistry (IHC) staining. In addition, the levels of enzymatic antioxidants and malondialdehyde were also measured in the wound tissue homogenates. Wounds treated with extracts (PL, PR, AL, and AR) showed significantly faster healing (p < 0.05) compared to untreated and control groups (SH, VD, and FD). Histological analysis among MP-treated groups revealed better re-epithelialization, higher collagen deposition, enhanced fibronectin content and fibroblast cells, and higher fiber transformation from collagen-III to collagen-I, accompanied with a significant surge in enzymatic antioxidant activities and a decline in lipid peroxidation. MP has antioxidant effects that may enhance wound healing in the rat model.     

Synthesis of Some New Benzimidazole–Thiazole Derivatives as Anticancer Agents

4‐(1H‐benzo[d]imidazol‐2‐yl)thiazol‐2‐amine and its 1‐methyl derivative ( 1 ) were reacted with different reagents such as acid anhydrides, malononitrile, chloroacetyl chloride, and aromatic aldehydes to produce the corresponding benzimidazole products 2 , 3 , 4 , 5 , 6 , 7 , 8 , 9 , respectively. Also, 2‐chloro‐N‐(4‐(1‐methyl‐1H‐benzo[d]imidazol‐2‐yl)thiazol‐2‐yl) acetamide ( 6 ) was reacted with diaminoethane, ortho‐substituted aniline, thioglycolic acid, thiosemicarbazide derivatives, secondary amines, and potassium isothiocyanate to afford the corresponding derivatives 10 , 11 , 12 , 13 , 14 , 15 , 16 , 17 , respectively. The cytotoxic activity of some newly synthesized derivatives was studied against two different cell lines HepG2 and PC12. Compounds 9 and 15b showed promising anticancer activity against both types of the tested cancerous cell lines.     

Effect of CdSe quantum dots doping on the switching time,localised electric field and dielectric parameters of ferroelectric liquid crystal

A systematic study highlighting the effect of cadmium selenide quantum dots (CdSe QDs) with varying concentrations of 0.05, 0.10 and 1.0 wt% doping on the electrooptical and dielectric parameters of ferroelectric liquid crystal (FLC) is presented. No considerable change is observed in phase transition temperature and tilt angle with CdSe QDs doping at lower and higher dopant level. Substantial enhancement of localised electric field at higher doping level (1.0 wt%) of CdSe QDs manifested the ≈48% reduction in the switching response of FLC nanocolloids at 30°C. Reduction in the spontaneous polarisation, dielectric constant and absorption strength could be attributed to the antiparallel correlation among dopant and matrix molecules, ion capturing in the capping additive layer and enhancement of the rotational viscosity of the nanocolloids, respectively. Goldstone mode relaxation frequency is found to be decreased with doping up to 0.10 wt% concentration and showed reverse effect at higher QDs concentration. QDs doping effect on the photoluminescence intensity is also discussed.