The reaction of cyanoacetyl hydrazine (1) with the -haloketones 2a-2c in 1,4-dioxane afforded the hydrazidehydrazone derivatives 3a-3c. The latter products were used in a series of heterocyclization to give 1,3,4-oxadiazine, 1,2,4triazine and pyrazole derivatives. All compounds synthesized through this work are new products and their antitumor evaluation towards three human tumor cell lines rep...

Abstract New system compromising of chitosan nanoparticles encapsulated pre-synthesized selenium in the presence 5-fluorouracil was successfully prepared and used for cancer antiproliferation. Selenium were synthesized using ascorbic acid as reducing agent under mild condition. Chitosan via ionic gelation technique sodium tri-polyphosphate. Characterization carried out FTIR, TEM, XRD, TGA dynam...

Argentatins A–C (1–3), the major cycloartane-type triterpenoids of guayule resin, a byproduct commercial rubber production, were converted into their pyrimidine (7–12), thiazole (13–15), and indole (16–18) analogues by molecular hybridization approach. The cytotoxic activities these fused heterocyclic 7–18 compared with those argentatins (1–3) against panel three sentinel human cancer cell line...

BACKGROUND Breast cancer is one of the most dreading types of cancer among women. Herbal medicine has becoming a potential source of treatment for breast cancer. Herbal plant Dillenia suffruticosa (Griff) Martelli under the family Dilleniaceae has been traditionally used to treat cancerous growth. In this study, the anticancer effect of ethyl acetate extract of D. suffruticosa (EADs) was examin...

Pyranoxanthones 6-8 were obtained by dehydrogenation of the respective dihydropyranoxanthones 3-5 with DDQ in dry dioxane. Two prenylated xanthones 10,11 were obtained from the reaction of 1-hydroxyxanthone (9) with prenyl bromide in alkaline medium, or by condensation of xanthone 9 with isoprene in the presence of orthophosphoric acid. The structural elucidation of the two new compounds 6,11, ...

Human breast cancers cells overexpressing HER2/neu are more aggressive tumors with poor prognosis, and resistance to chemotherapy. This study investigates antiproliferation effects of anthraquinone derivatives of rhubarb root on human breast cancer cells. Of 7 anthraquinone derivatives, only rhein showed antiproliferative and apoptotic effects on both HER2-overexpressing MCF-7 (MCF-7/HER2) and ...

Over the last decade, there has been growing interest in developing novel nanoparticles (NPs) for biomedical applications. A safe-by-design approach was used in this study to synthesize biocompatible iron oxide NPs. The size of the particles obtained was ~100 nm. Although these NPs were significantly (P<0.05) internalized in MCF-7 (human breast adenocarcinoma cell line) cells, no adverse effect...

Andrographolde is the major secondary metabolite from the plant Andrographis paniculata. It has been found to show cytotoxic activity. To improve the efficacy on cytotoxic activity, a series of new sulfonyl derivatives have been synthesized by structural modifications of the andrographolide at C-2 position. All the derivatives were tested for their cytotoxic activity against human small lung ca...

Co-delivery approach has been recommended to reduce the amount of each drug and to achieve the synergistic effect for cancer treatment. CUR and SF have antitumor effects, but their application is limited because of their low water solubility and poor oral bioavailability. To improve the bioavailability and solubility of SF and CUR, we performed an innovative co-delivery of SF and CUR with magne...

The marine environment represents approximately half of the global biodiversity and could provide unlimited biological resources for the production of therapeutic drugs. Marine seaweeds comprise few thousands of species representing a considerable part of the littoral biomass. Extracts of the Cystoseira indica and Cystoseira merica were subjected to phytochemical and cytotoxicity evaluation. Th...