Quercetin, a ubiquitous flavonol, represents a promising leading drug for development of new chemotherapeutic agents. However, its limited cytotoxicity to cancer cells hampers its clinical use. In order to obtain novel quercetin derivatives with superior cytotoxicity, seven alkylated quercetin derivatives were synthesized. Solubility of these derivatives was determined by turbidimetry. Cytotoxi...

In a systematic effort to identify a potent antiproliferative agent, four complexes of vanadium containing maltol and deferiprone ligands were synthesized and evaluated for their cytotoxic activity against five human and animal cancer cell lines, including human breast cancer cells (MCF-7), human cervix epithelial carcinoma (HeLa), human colon cancer cell line (HT-29), human leukemia cell line ...

quercetin, a ubiquitous flavonol, represents a promising leading drug for development of new chemotherapeutic agents. however, its limited cytotoxicity to cancer cells hampers its clinical use. in order to obtain novel quercetin derivatives with superior cytotoxicity, seven alkylated quercetin derivatives were synthesized. solubility of these derivatives was determined by turbidimetry. cytotoxi...

Background: Parthenolide is major sesquiterpene lactones present in Tanacetum parthenium (L.) Sch.Bip. (feverfew).  This compound is known as herbal active principals with potential use in pharmaceutical and medicine. In order to solubility improving, analogue of Parthenolide, aminopropyl theoxy silane -mesoporous silica of Parthenolide, was synthesized as well. In this study, it was e...

the cypress family, cupressaceae, has a global dispersion. currently, endophytic microorganisms from plants are being investigated for their diversity and bioactivities. here, we aimed at exploration and characterization of cultivable endophytic fungi from foliar tissues of cupressaceae, i.e. cupressus arizonica, c. sempervirens var. cereiformis, c. sempervirens var. fastigiata, juniperus excel...

Calcitriol is a potent antiproliferative agent against various tumour cells in vitro. Here, the results of a study on vitamin D compounds (calcitriol's analogues PRI-1906 and PRI-2191) as potential agents in combined antitumour therapy in vitro are presented. Applying antiproliferative SRB and MTT assays, the growth inhibitory effects of the vitamin D compounds, applied alone or in combination ...

Betulinic acid, a very promising anti-melanoma agent, has very low water solubility that causes low bioavailability. To overcome this inconvenience, a highly water-soluble cyclodextrin was used (octakis-[6-deoxy-6-(2-sulfanyl ethanesulfonic acid)]-γ-cyclodextrin). The complex was physico-chemically analyzed using differential scanning calorimetry (DSC), X-ray and scanning electron microscopy (S...

Sertraline, a selective serotonin reuptake inhibitor, is a widely used antidepressant agent. Here, we show that sertraline also exhibits antiproliferative activity. Exposure to sertraline leads to a concentration-dependent decrease in protein synthesis. Moreover, polysome profile analysis of sertraline-treated cells shows a reduction in polysome content and a concomitant increase in 80S ribosom...

Multi-target drug design, in which drugs are designed as single molecules to simultaneously modulate multiple physiological targets, is an important strategy in the field of drug discovery. QT-011, a tamibarotene-furoxan derivative, was here prepared and proposed to exert synergistic effects on antileukemia by releasing nitric oxide and tamibarotene. Compared with tamibarotene itself, QT-011 di...

In response to a given stimulus, usually a number of cytokines are secreted simultaneously by the immune system. Whether these cytokines are meant to function as a single agent or in combination with others is not understood. Tumor necrosis factor (TNF) has been shown to exhibit antiproliferative effects against a wide variety of tumor cell lines in vitro. In the present report, we investigated...