Letters in Drug Design & Discovery - Volume 13, Issue 2, 2016

Plant growth regulators with the suitable concentrations had obvious effects on the accumulation of indole alkaloids in Catharanthusroseus cells#142;Four new compounds were synthesized as plant growth regulators and the accumulation effects of indole alkaloids in Catharanthusroseus cells were determined. Furthermore, some of them had the ability of promoting the accumulation of catharanthineandajmalicine in Cath Read More

Synthesis, molecular docking study, and cytotoxic activity of a new group of 1,3,5-triaryl pyrazole derivatives were be studied. The antiproliferative activity of the final compounds were examined in MCF-7, AGS, HT-29 and NIH3T3 cell lines by MTT assay, using different concentrations of each compound to determine their IC50 . The cytotoxic activity of paclitaxel and doxorubicin were evaluated as positive controls. All compoun Read More

The research on protein phosphorylation by kinases in various cellular processes is increasing significantly for the identification of kinase-based drugs. This is due to the fact that several kinasebased (anticancer) drug candidates have already been approved for clinical use and some are undergoing clinical trials as well. This scenario has amplified the momentum for the discovery of kinase-based drugs for other health pr Read More

Objective: This study aimed to elucidate the antibacterial properties and therapeutic effect in refractory diabetic wound healing of a NanoAg-epidermal growth factor sustained-release carrier(NanoAg-EGF). Methods: as previous publishing, the sustained-release carrier of NanoAg-EGF can be conducted. The antibacterial properties and therapeutic effects of NanoAg-EGF were determined through in vitro bacterial growth in Read More

A series of 4-phenylthieno[2,3-e][1,2,4]triazolo[4,3-a]pyrimidine-5(4H)-ones (5a–p) with triazole or other heterocyclic substituents (6–11) was synthesized and the compounds were evaluated for their anti-inflammatory activity using the xylene-induced ear-edema test. Pharmacological analyses showed that the compound 4-(4-chlorophenyl)thieno[2,3-e][1,2,4]triazolo[4,3-a]pyrimidine- 5(4H)-one (5m) exhibited the great Read More

A series of novel spiro-piperidinyl pyrazolones were synthesized starting from the commercially available ethyl nipecotate. The Boc protected ethyl nipecotate was reacted with 5-bromo-2-furaldehyde in the presence of LDA to afford the β -hydroxy ester which was converted to the β -keto ester by oxidation using manganese dioxide. Furthermore, β-keto ester was treated with hydrazine to form the spiro-piperidinyl pyrazolone sc Read More

The qualitative relationship between in vitro Caco-2 cellular transport and in vivo drug permeability allow using Caco-2 cell assay for intestinal absorption studies. In this work, atom-based bilinear indices and multiple linear regression (MLR) are applied to obtain models useful for the prediction of Caco-2 cell absorption. Making use of a previously reported database, we obtain four statistically significant MLR models, th Read More

Natural products are recent emerging effective agents against many chronic human diseases. Curcumin (diferuloylmethane), the active constituent of turmeric (Curcuma longa), has gained much interest as a plant-based compound with pleiotropic biological activities. Curcumin has been shown to possess significant anti-oxidant, anti-carcinogenic, anti-inflammatory, and anti-microbial effects. Although the history of curcumin goe Read More

A series of new N’-(arylidene)-2-[(1-(4-nitrophenyl)-1H-1,2,4-triazol-3-yl)oxy]acetohydrazide derivatives (1- 16) were prepared and tested for theira ntifungal activity against six plant pathogens, three human pathogens and two nonpathogen microorganisms. The target compounds were obtained with a multi-step reaction starting from 4- substitutedarylhydrazine derivatives and the structures of final compounds have been elucida Read More

Tuberculosis remains a major health problem due to drug resistance and co-infection. Discovery of new drugs to counter tuberculosis is an urgent need. Multi-targeting strategy is one among the effective approach to combat the disease. Multi-targeting has minimal adverse effects. It is also difficult for Mycobacterium tuberculosis to survive and evolve into more drug-resistance strains in case of multi targeting. Lipases Rv018 Read More