Letters in Drug Design & Discovery - Volume 9, Issue 10, 2012

A series of 2,3,5-trisubstituted and 1,2,3,5-tetrasubstituted indoles is synthesized by Fisher or Bischler method, followed by alkylation with an appropriate alkyl or aryl halide. Two compounds exhibit non-competitive antagonism towards GluK1 and six – towards GluK2 receptor. The values of IC50 are in micromolar range. The investigated compounds belong to the most active GluK1 non-competitive inhibitors and are the first Read More

Vascular endothelial growth factor (VEGF) and its receptor tyrosine kinase VEGFR-2 are critical regulators of angiogenesis. The blockage of VEGFR-2 signaling by small molecule inhibitors has been shown to inhibit angiogenesis and tumor progression. The article describes the development of a robust pharmacophore model and the investigation of structure activity relationship analysis of benzoquinone derivatives reported for V Read More

Diabetes mellitus, a chronic condition caused by defects in insulin secretion, or action, or both, is a group of metabolic disorders whose complications can contribute significantly to ill health, disability, poor quality of life and premature death. From the three main types of diabetes, Type 2 is by far the most common, accounting for about 90% of cases worldwide. Studies on the role of protein tyrosine phosphatase 1B Read More

Selected adamantanyl purines and pyrimidines 1-10 were synthesized. These compounds were evaluated for cytotoxic activity against NCI-60 DTP human tumor cell line screen. N9-(3'-Adamantan-1-yl)-4'-hydroxy(benzyl)-2- amino-6-chloropurine, 3 and N9-[(3'-(Adamantan-1-yl)-4'-(2'',3'',4''-trifluorobenzyloxy)]benzyl-2-amino-6-chloropurine, 6 elicited significant cytotoxic activity with GI50 values in the 1–10 μM range for selec Read More

In obtaining some new cytotoxic and chemopreventive agents with potent antiproliferative activity against cancer cells, a series of new β-isatin aldehyde-N,N'-thiocarbohydrazone, bis-β-isatin thiocarbohydrazones, bis-β-isatin carbohydrazones, N,2-bis(thiophen-2-ylmethylidene) thiocarbohydrazone and N,2-bis(thiophen-2-ylmethylidene) carbohydrazone derivatives was synthesized by microwave oriented reaction Read More

Novel 3,5-disubstituted 1,2,4-oxadiazoles 4a-4j were prepared from commercially available chlorosalicylaldehyde and screened for their cytotoxicity properties using brine shrimp (Artemia salina) bioassay and compared with the standard podophyllotoxin. The oxadiazoles 4a, 4c, 4e and 4h exhibited cytotoxicity activity in the series.

Fourteen novel compounds were obtained and their chemical structures were established by 1H-NMR and IR spectra as well as elemental analyses. As one of the most important factors determining the changes of activity of respective fluorophenyl and iodophenyl derivatives, one should consider the volume of halogen substituent and its influence on the lipophilicity of the entire molecule.

The aim of this work was to synthesize a series of compounds to study their antimycobacterial potential. Eight compounds were found to be most active with minimum inhibitory concentration of less than 6μM and were more active than Isoniazid (INH) against Mycobacterium tuberculosis H37Rv (MTB). Compounds with electron withdrawing group substituted on the aryl ring were showing better activity. Among the fifteen n Read More

With the ultimate purpose of finding out the structural features that are relevant for MAO inhibitory activity and selectivity towards MAO-B isoform, a series of compounds encompassing a β-nitrostyrene moiety was designed and the in vitro inhibitory activity was evaluated. In the present work, we report the synthesis and the pharmacological evaluation of a series of functionalized derivatives of β-methyl-β-nitrostyrene with disti Read More

The series of 3,4–dihydropyrimidin–2-ones (DHPMs) were synthesized using recyclable silica supported RhCl3 as heterogeneous catalyst and evaluated for anti-neuroinfammatory effect in microglia cells. Among the DHPMs tested, compounds 4g, 4j and 4v strongly inhibited LPS-induced nitric oxide (NO) production with IC50 value of 67.32, 46.01 and 41.31 μM in the microglia cells. Also, compounds 4g, 4j and 4v significan Read More

Hydroxysafflor Yellow A (HSYA) is one of the most important active ingredients of Carthamus tinctorius L, and has long been widely used in the treatment of cardiovascular diseases in China. The purpose of this study was to evaluate the role of HSYA in protecting the kidney against ischemia/reperfusion injury (IRI). Male Wistar albino rats (200-250 g) were unilaterally nephrectomized and subjected to 45-min renal isc Read More