Letters in Drug Design & Discovery - Volume 12, Issue 1, 2015

The discovery of promising targets for anticancer drug development has emerged with many potential enzymes. Among these, the aurora family of kinases has become a very lucrative target with some potential inhibitors in its arsenal. Recent findings show that targeting aurora B itself is sufficient to exhibit anticancer activity. When compared with other anticancer targets, aurora B has a very limited number of specific inh Read More

We report herein a feasible study concerning the design, synthesis, structure and in vitro antimycobacterial activity of new phenanthroline derivatives with p-halo-benzoyl skeleton. The preparation is straight and efficient, involving an N-alkylation reaction of 1,7- phenanthroline. The antimycobacterial agents have been prepared in good yields and purity. The antimycobacterial activity of the synthesized compounds w Read More

Novel imatinib amide derivatives (a1-28, b1-9) were synthesized and evaluated for their biological activities. All compounds were characterized by 1H NMR, MS and elemental analysis. Among all the derivatives, compounds a4, a10, a21, b1 and b2 displayed the most significant ability of inhibiting K562 cell proliferation with the IC50 values of 0.67, 0.66, 0.65, 0.59 and 0.62 µM, respectively, indicating that these compound Read More

A series of 2-amino-5-(4-(benzyloxy)benzyl)thiophene-3-carboxylic acid derivatives was designed and synthesized. The derivatives were evaluated for antitubercular activity against M. tuberculosis ATCC 27294 using the Microplate Alamar Blue Assay (MABA). Among them, compound 8b exhibited the most potent activity with MIC value of 1.9 µM.

A series of novel benzimidazole-pyridine-piperidine hybrids was synthesized in good yields and characterized by spectral and elemental analyses. The compounds 4a-h and 5a-c were evaluated for their in vitro antibacterial activity against gram-positive organisms viz., Bacillus subtilis, Staphylococcus aureus, Staphylococcus epidermidis, gramnegative organisms viz., Escherichia coli, Pseudomonas aeruginosa, Klebsiella Read More

Treponema pallidum, a Gram negative bacterium, causes chronic disease syphilis, a sexually transmitted disease. T. pallidum penetrates dermal micro abrasions or intact mucous membranes resulting in varieties of symptoms. The complete genome for T. pallidum was sequenced, which contains approximately 1,090 genes encoding approximately 1,041 proteins. These open reading frames account for a large number of Read More

In this contribution, we attempted to design novel inhibitors of the serine/threonine-protein kinase Chk1. After studying the interaction of Chk1 ATP binding site with known inhibitor C39, we created seven modified C39-based molecules in order to achieve higher binding potentials. Of those, modified molecules 2, 4, 6 and 7 (MD2, MD4, MD6 and MD7) were selected to be assembled in three new molecules, originating MD8, M Read More

The Hsp90/Cdc37 (heat shock protein 90; cell division cycle 37) interaction is a promising target for anticancer candidate drug development. The purpose of this research is to establish a screening method for anti-cancer candidate compounds based on the Hsp90/Cdc37 interaction model in vitro by Split Renilla luciferase protein fragment-assisted complementation bioluminescence technology. The parameters influencing the Read More

The bornyl ester derivatives of non-steroidal anti-inflammatory drugs (NSAIDs) including naproxen, ketoprofen and flufenamic acid, were synthesized and their transdermal permeation efficiency and pharmacological activity were determined. The bornyl NSAID esters exhibited more than 10-fold increase of permeation efficiency across mice skin than parent NSAIDs. The preliminary biological and pharmacological eva Read More

The optimized synthesis of benzidronate involves the reaction of phenylacetic acid with 3 equivalents of phosphorus trichloride and 1 equivalent of phosphorous acid in methanesulfonic acid at 85 °C followed by hydrolysis, pH adjustment and purifications. The positive effect of phosphorous acid on the yield is a novel observation and is probably limited to this model. The heap of our experimental data obtained by varying the mol Read More