The 3-D morphology of doxorubicin (DOX)–loaded liposomes with a size of circa 100 nm was characterized by atomic force microscopy in an aqueous environment. Prolate liposomes appear in accordance with linear expansion of DOX fiber bundles precipitated inside liposomes. Oblate and concave liposo...

We report the design, synthesis and biological evaluation of 17 novel 8-aryl-2-morpholino-3,4-dihydroquinazoline derivatives based on the standard model of DNA-PK and PI3K inhibitors. Novel compounds are sub-divided into two series where the second series of five derivatives was designed to have...

Lung cancer is the leading cause of cancer death worldwide. To overcome the toxic side effects and multidrug resistance (MDR) during doxorubicin (DOX) chemotherapy, a urokinase plasminogen activator receptor (uPAR) targeting U11 peptide decorated, pH-sensitive, dual drugs co-encapsulated nanopar...

In recent years, polysaccharide-decorated superparamagnetic iron oxide nanoparticles (SPIONs) have gained attention in the field of “nanotheranostics” with integrated diagnostic and therapeutic functions. Carboxymethyl Assam bora rice starch-stabilized SPIONs (CM-ABRS SPIONs), synthesized by c...

Drug efflux transporters, in particular P-glycoprotein (Pgp), limit the success of chemotherapy. We previously found that synthetic doxorubicin conjugated with nitric oxide (NO)-releasing group overcomes resistance by inducing a NO-mediated inhibition of Pgp. Here we produced the first liposomal...

Aggregation of thermoresponsive chains to form mesoglobules is a promising way to make nanoaggregates useful as drug carriers. Here, we present for the first time, a route for the formulation of mesoglobules that may be used as polymer carriers for doxorubicin (DOX). For this purpose, a thermore...

Acidic pH in the tumor microenvironment is associated with cancer metabolism and creates a physiological barrier that prevents from drugs to penetrate cells. Specifically, ionizable weak-base drugs, such as doxorubicin, freely permeate membranes in their uncharged form, however, in the acidic tu...

Doxorubicin (dox) is one of the first-line drug in osteosarcoma treatment but its effectiveness is limited by the efflux pump P-glycoprotein (Pgp) and by the onset of cardiotoxicity. We previously demonstrated that synthetic doxs conjugated with a H2S-releasing moiety (Sdox) were less cardiotoxi...

The rhenium(I) carbonyl bromide complex, [ReBr(CO)3(HL)], of the ligand derived from 2,4-dihydroxybenzaldehyde and 4-hydroxybenzoic acid hydrazide (HL), has been prepared. HL and its complex have been characterized by elemental analysis, MS, IR, UV–Vis and 1H NMR spectroscopic methods. The stru...

Enhanced ultraviolet radiation (UV) is an important environmental factor that may cause reductions in the growth and productivity of plants. In the present work we studied the response to UV-B radiation in leaves of the model legume Lotus japonicus. After UV-B treatment, induction of phenyalanin...

Four new triphenyltin(IV) acylhydrazone compounds of the type Ph3SnCH2CH2CONHN=R (where Ph = phenyl; R = isopropyl, isobutyl, cyclopentyl and cyclooctyl) were synthesized and characterized by elemental analysis, infrared spectrum (IR), nuclear magnetic resonance spectrum (NMR) and mass spectrum ...

When the overidentifying restrictions of the constant-effect linear instrumental variables model fail, common IV estimators converge to different probability limits. I characterize the estimands of two stage least squares, two step GMM, and limited information maximum likelihood as functions of ...

The binuclear platinum(IV) complexes [NBu4]2[PtIV2(μ-Cl)2(C6F5)4Cl4] (2) and [PtIV2(μ-C8H6N4)2(C6F5)4Cl4] (4) have been synthesized by oxidative addition of chlorine to the binuclear platinum(II) species, but [NBu4]2[PtIV2(μ-OH)2(C6F5)4Cl4] (3) has been synthesized by substitution of the chlo...

Three new metal complexes {M=Pd(II) or Pt(II)} containing the ligand 3-aminopyrrolidine were prepared. The compounds were characterised by IRFT, and 1H, 13C and 195Pt NMR spectroscopies. Crystal structures of the palladium complexes of formulae cis-[PdCl2(pyrr)] and trans-[Pd(pyrr)2](ClO4)2 were...

Over 20 new and easily prepared diamines were screened for the asymmetric Morita–Baylis–Hillman reaction. Chiral non-racemic 3-(N,N-dimethylamino)-1-methylpyrrolidine was found to promote efficiently the reaction of methyl vinyl ketone and substituted benzaldehydes. Enantiomeric excesses up to...

The resolution of 3-aminopyrrolidine 1, a versatile key intermediate for chiral pharmaceuticals, via diastereomeric salt formation was investigated. The resolution conditions were optimized focusing on an industrial-scale production to afford enantiopure (R)-1, while (S)-methoxy-2-phenylacetic a...

Pyrazine diazohydroxide (NSC 361456) (PZDH) was selected for further development after demonstrating more stability than its parent compound and significant antitumor activity in a number of in vivo tumor models. Its proposed mechanism of action is through the formation of DNA adducts via the re...

Diazohydroxide is a new antitumor agent being considered for clinical trial. A sensitive and specific assay for diazohydroxide in physiological media, plasma and blood has been developed based on conversion of diazohydroxide to 2-chloropyrazine in the presence of strong hydrochloric acid. The 2-...

The purpose of this study was to develop a method for the stereoselective analysis of thioridazine-2-sulfoxide (THD-2-SO) and thioridazine-5-sulfoxide (THD-5-SO) in culture medium and to study the biotransformation of rac-thioridazine (THD) by some endophytic fungi. The simultaneous resolution o...

An experimental and in silico quantitative structure-activity relationship (QSAR) approach was applied to assess the environmental fate and effects of the antipsychotic drug Thioridazine (THI). The sunlight-driven attenuation of THI was simulated using a Xenon arc lamp. The photodegradation reac...