Letters in Drug Design & Discovery - Volume 12, Issue 10, 2015

In this study, we tried to improve the anticancer properties of two potential cytostatic agents based on benzo[c]fluorene, benfluron and dimefluron, by the synthesis of their C-7 derivatives. In the new derivatives, we observed the effect in Ehrlich tumour-bearing mice as well as in human MCF-7, BT-549 and MDA-MB-231 cells. All of the compounds tested showed a strong inhibitory effect in vitro. When tested in vivo, their systemic Read More

A series of simple isatin Schiff bases were synthesized through the condensation reaction. These isatin Schiff bases were characterized by NMR and MS, and the structure was discussed. Then, the cytoprotective and anti-tumor activities of these compounds were evaluated. The results show that several compounds show protection activity on the apoptosis of PC12 cells induced by H2O2, which are more effective than that of (±) α Read More

Chalcones and Mannich bases are bioactive compounds and known with their cytotoxicities. α,β-Unsaturated ketones are reported with their alkylating potential to cellular thiols thereby inducing cytotoxicities. In this study; Mannich bases (MT2-MT7), which may generate two additional alkylating centers comparing with starting compound 2-(4-hydroxybenzylidene)-2,3-dihydroinden-1- one MT1, were designed and synthe Read More

In this work, a series of N-substituted isatin derivatives was synthesized by different reactions. The synthesized isatin derivatives were characterized by NMR, MS and elemental analysis. Then the anti-tumor activities of these compounds were evaluated through the cytotoxicity against A549 and P388 cell line test. The results show that several compounds show much higher anti-tumor activity than that of isatin, and there is an ev Read More

Identification of compounds which can inhibit the activity of urease enzyme is an important approach towards the treatments of peptic ulcer, urolithiasis, and other urease associated disorders. This manuscript describes the in vitro urease inhibitory activity of different derivatives of phenols, heterocyclic compounds, thiols, quinone, tosylphenyl alanine, sulfonyl cyanides, phenyl acetoacetate, and thiamines (1-14). Am Read More

The pseudo-trisaccharide allosamidin 1 is a potent inhibitor of all family 18 chitinases, and it is confirmed to have insecticidal and antifungal activities. However, the synthesis of allosamidins is very difficult, and it is a challengeable subject. Allosamidins were synthesized in solid/liquid phase and total solid phase, respectively. Solid/liquid-phase method realizes the partial solid-phase synthesis of allosamidins. Total solid-p Read More

The brain serotonin (5-HT) and dopamine (DA) systems are targets for many clinically effective antidepressants. Here, we studied the effects of acute administration of a new potential antidepressant drug, 8-(trifluoromethyl)-1,2,3,4,5 - benzopentathiepin-6-amine hydrochloride (TC-2153), on the concentration of 5-HT and DA as well as their main metabolites, 5-hydroxyindoleacetic (5-HIAA) and homovanillic acids (HVA), in the Read More

Acetylcholinesterase (AChE) is an attractive target of drugs for Alzheimer’s disease (AD). A series of novel synthesized flavonoid derivatives have been reported as potent AChE inhibitors, but the lack of structure-AChE inhibitory activity relationships hampers the design of specific and selective flavonoid derivatives. In this study, 3D-quantitative structure activity relationship (3D-QSAR) models of 90 flavonoid derivatives as AChE i Read More

Fluoroquinolones are well known and among most promising nitrogen containing heterocyclic compounds depicting broad spectrum and potent anti-infective activities. Numerous fluoroquinolone derivatives have been found to possess considerable favorable properties such as excellent bioavailability, good tissue penetrability and low toxic effects which attract the extensive research endeavors worldwide. With a better u Read More

Drugs comprising a heterocyclic system show widespread therapeutic impact such as antimicrobial, antidepressant, antihypertensive, and anticancer activity. We describe herein computational studies that support the promising biological activity of four new compounds (5, 6, 10 and 13). The wild-type and mutant phosphatidylinositol-4,5-bisphosphate 3-kinaseα (PI3Kα) proteins were used as models to explore the pot Read More

A series of 2´-hydroxy-4´,6´-diisoprenyloxychalcone derivatives were synthesized and evaluated for inhibitory activities against CDC25B and PTP1B. The results displayed the most of them showed inhibitory activities against CDC25B (IC50=1.19–14.20 µg/mL) and PTP1B (IC50= 1.26–8.44µg /mL), respectively. Moreover, compound 2h displayed the most CDC25B and PTP1B inhibitory activity in vitro with IC50 values of 1.19 and 1.26 Read More