Our objective was to assess whether the total area under the curve (AUC) of high-dose cyclophosphamide (CPA), combined with cisplatin and 1,3-bis(2-chloroethyl)-1-nitrosourea, could be predicted from its AUC on the first day of treatment. We reviewed the AUC of CPA in 470 patients who underwent pharmacokinetic monitoring of the drug. All patients received the same high-dose regimen of CPA, cisp...

Hyperthermia has been shown to increase the cytotoxic effect of certain cancer chemotherapeutic agents in vitro and in vivo. It is not known whether the combination of hyperthermia plus these chemotherapeutic drugs will also increase the tox icity of the drugs. This study was undertaken to evaluate the toxic effects of 1,3-bis(2-chloroethyl)-i -nitrosourea combined with hyperthermia on normal m...

Antimalarial chloroquine (CQ) prevents haematin detoxication when CQ-base concentrates in the acidic digestive vacuole through protonation of its p-aminopyridine (pAP) basic aromatic nitrogen and sidechain diethyl-N. CQ export through the variant vacuolar membrane export channel, PFCRT, causes CQ-resistance in Plasmodium falciparum but 3-methyl CQ (sontochin SC), des-ethyl amodiaquine (DAQ) and...

BACKGROUND In the past few years, increased resistance of microorganisms towards antimicrobial agents become a serious health problem, so there is a need for the discovery of new antimicrobial agents. On the other hand, bis-pyrimidines possess various types of biological activity. In view of this, in the present study we have designed and synthesized a new series of bis-pyrimidine acetamides by...

Uncompetitive N-methyl-d-aspartate (NMDA) receptor antagonists with fast off-rate (UFO) may represent promising drug candidates for various neurodegenerative disorders. In this study, we report that bis(propyl)cognitin, a novel dimeric acetylcholinesterase inhibitor and γ-aminobutyric acid subtype A receptor antagonist, is such an antagonist of NMDA receptors. In cultured rat hippocampal neuron...

The present study evaluated a new concept of combined scaffolds as a promising bone replacement material for patients with a bone tumour or bone metastasis. The scaffolds were composed of hydroxyapatite doped with selenium ions and a biodegradable polymer (linear or branched), and contained an active substance-bisphosphonate. For this purpose, a series of biodegradable polyesters were synthesiz...

Nowadays, obesity becomes a serious global problem, which can induce a series of diseases such as type 2 diabetes mellitus, cancer, cardiovascular disease, metabolic syndrome, and stoke. For the mechanisms of diseases, the hedgehog signaling pathway plays an important role in body patterning during embryogenesis. For this reason, smoothened homologue (Smo) protein had been indicated as the drug...

The bispectral index (BIS, Aspect Medical Systems, Inc. Newton, MA) is becoming the gold standard for assessing depth of anesthesia in adult patients. Indeed, BIS values are highly correlated with the concentration of hypnotic drugs such as propofol or sevoflurane (1–8). The BIS is derived from a large database of EEG traces obtained in adult patients under various conditions of anesthesia (9)....

Chalcone-derived pyrimidine is a well-known heterocyclic compound that commonly present in ribonucleic acid (RNA) and deoxyribonucleic (DNA) bio-isosteres. Pyrimidine derivatives are effective both the electronic industry drug industries. This review highlights synthesis of pyrimidines, namely mono-pyrimidine, bis-pyrimidine, fused pyrimidine, symmetric, asymmetric via one-pot two-pot methods. ...