Search results for " antiproliferative activity"

Synthesis of the new ring system 6,8-dihydro-5H-pyrrolo[3,4-h]quinazoline

2009

Abstract A convenient synthesis of the pyrrolo[3,4- h ]quinazoline ring system is reported. Our synthetic approach consisted of the annelation of a pyrimidine ring to an isoindole moiety using tetrahydroisoindole-4-ones as building blocks. The antiproliferative activity of the new compounds was investigated and one of them showed antitumor activity against all the 59 tested cell lines at micromolar concentrations (1.46–18.4 μM).

The size of aryl linker between two polyaza-cyclophane moieties controls the binding selectivity to ds-RNA vs ds-DNA

2013

Aryl-linked (pyridine- vs. phenanthroline-) bis-polyaza pyridinophane scorpiands PYPOD and PHENPOD strongly bind to the double stranded DNA and RNA, whereby very intriguing RNA over DNA selectivity is finely tuned by aryl-linker length and aromatic surface. Moreover, PYPOD and PHENPOD dimer formation at high compound/polynucleotide ratios is highly sensitive to the fine interplay between the steric and binding properties of compound-dimers and the DNA minor groove/RNA major groove. That is demonstrated by significantly different induced CD spectra, which allow spectroscopic differentiation between various DNA/RNA secondary structures. A significantly higher (micromolar) antiproliferative ef…

Synthesis, antiproliferative activity, and mechanism of action of new benzamido derivatives

2011

The cinnamoyl anthranilamides represent a class of biological active substances of great importance in medicinal chemistry. Moreover, despite their wide range of biological activities, a review of the literature revealed that no anticancer activity is described for this kind of substances. Starting from the 2-cinnamamido-5-iodobenzamide, resulted able to inhibit the leukemic cell line K-562 proliferation with a percent of inhibition of 74% at 10M concentration, we undertake the following structural modifications on cinnamamidobenzamide skeleton: the introduction of various substituents both on the benzamido and the cinnamamido moieties, the substitution of olefinic bond with the ethane, et…

SYNTHETIC AND BIOLOGICAL EVALUATION OF SOME NEW 2-CINNAMAMIDOBENZAMIDES AS POTENTIAL ANTAGONIST OF THE HDM2-P53 PROTEIN-PROTEIN INTERACTIONS

2008

Essential oils of Salvia bracteata and Salvia rubifolia from Lebanon: Chemical composition, antimicrobial activity and inhibitory effect on human mel…

2009

Aim of the study: Salvia bracteata Banks et Sol. and Salvia rubifolia Boiss. are known in folk medicine of Lebanon for the treatment of microbial infections, cancer, urinary and pulmonary problems. In the present study the chemical composition and antimicrobial activity of essential oils from aerial parts of Salvia bracteata and Salvia rubifolia collected in Lebanon were evaluated. The oils were also tested for their potential antiproliferative effects against M14 human melanoma cells. Material and methods: The oils were studied by GC and GC-MS and their antibacterial activity (MIC and MBC) was tested against ten bacteria species using the broth dilution method. The inhibitory effect on hum…

New benzothieno[3,2-d]-1,2,3-triazines with antiproliferative activity: synthesis, spectroscopic studies, and biological activity.

2014

New benzothieno[3,2-d]-1,2,3-triazines, together with precursors triazenylbenzo[b]thiophenes, were designed, synthesized and screened as anticancer agents. The structural features of these compounds prompted us to investigate their DNA binding capability through UV–vis absorption titrations, circular dichroism, and viscometry, pointing out the occurrence of groove-binding. The derivative 3-(4-methoxy-phenyl)benzothieno[3,2-d]-1,2,3-triazin-4(3H)-one showed the highest antiproliferative effect against HeLa cells and was also tested in cell cycle perturbation experiments. The obtained results assessed for the first time the anticancer activity of benzothieno[3,2-d]-1,2,3-triazine nucleus, and…

2-Cinnamamido, 2-(3-phenylpropiolamido), and 2-(3-phenylpropanamido)benzamides: synthesis, antiproliferative activity, and mechanism of action

2013

Abstract Several new benzamides 4a–q were synthesized by stirring in pyridine the acid chlorides 3a–q with the appropriate anthranilamide derivatives 2a–g. Some of the synthesized compounds were evaluated for their in vitro antiproliferative activity against a panel of 5 human cell lines (K562 human chronic myelogenous leukemia cells, MCF-7 breast cancer cells, HTC-116 and HT26 colon cancer cells and NCI H460 non-small cell lung cancer cells).

Chemical and biological evaluation of cross-linked halloysite-curcumin derivatives

2020

Abstract Well designed and safe nano drug carrier systems are an important tool in biomedical applications. The combination of two or more drugs has been used in medicine both to enhance the therapeutic effect and to decrease the side effects of drugs. Biocompatible halloysite nanotubes, that possess two different surfaces, are a suitable nanomaterial for a simultaneous carrier and release of two drugs that can exert a synergistic effect against cancer cells. In this study, three curcumin derivatives and doxorubicin were loaded by supramolecular and covalent linkage at the lumen and external surface of the halloysite nanotubes. The obtained multifunctional systems were characterized by seve…

Chemical constituents and antiproliferative activity of Euphorbia bivonae

2011

Euphorbia is a genus of plants belonging to the family Euphorbiaceae, consisting of about 2160 species. This family occurs mainly in the Indo-Malayan region and tropical America. Euphorbia also has many species in non-tropical areas such as the Mediterranean area, the Middle East, South Africa, and southern USA. Phytochemical studies of species from the genus Euphorbia report the presence of skin-irritating and tumor-promoting diterpenoids, several macrocyclic diterpenoids with antibacterial, anticancer, PGE2-inhibitory, antifeedant, anti-HIV, and analgesic activities. Some of the Euphorbiaceae species are used in folk medicine for the treatment of skin diseases, gonorrhea, migraines, intes…

Direct chemical grafted curcumin on halloysite nanotubes as dual-responsive prodrug for pharmacological applications

2016

Covalently functionalized halloysite nanotubes (HNTs) were successfully employed as dual-responsive nanocarriers for curcumin (Cur). Particularly, we synthesized HNT-Cur prodrug with a controlled curcumin release on dependence of both intracellular glutathione (GSH) and pH conditions. In order to obtain HNT-Cur produgs, halloysite was firstly functionalized with cysteamine through disulphide linkage. Afterwards, curcumin molecules were chemically conjugated to the amino end groups of halloysite via Schiff's base formation. The successful functionalization of halloysite was proved by thermogravimetric analysis, FT-IR spectroscopy, dynamic light scattering and scanning electron microscopy. Ex…