Combinatorial Chemistry & High Throughput Screening - Volume 18, Issue 9, 2015

Antiandrogens bicalutamide, flutamide and enzalutamide etc. have been used in clinical trials to treat prostate cancer by binding to and antagonizing androgen receptor (AR). Although initially effective, the drug resistance problem will emerge eventually, which results in a high medical need for novel AR antagonist exploitation. Here in this work, to facilitate the rational design of novel AR antagonists, we studied Read More

Network pharmacology is an emerging technique, which integrates systems biology and computational biology to study multi-component and multi-targeted formulations. Ayurveda, the traditional system of Indian medicine, uses intelligent formulations; however, their scientific rationale and mechanisms remain largely unexplored. This paper presents the potential of network pharmacology to understand the rationale of a co Read More

The RNA helicase DHX9 is an ATP-dependent DExH box helicase that can unwind DNA and RNA. Much evidence has implicated DHX9 at multiple levels of gene expression regulation ranging from genome stability and replication, to transcriptional control and translation regulation. Its association with the EWS-FLI1 fusion product, as well as the finding that its suppression can be synthetic lethal with the BCL-2 family inhi Read More

Molecular docking studies of the designed two series (4a-l, 6a-l, 9 and 10) of novel substituted phosphorylated 1, 4-dihydropyridine and 1,2,3,4-tetrahydropyrimidine derivatives against the drug targets of DHFR from Bacillus cereus, LpxC from Pseudomonas aeruginosa, IDH from E. coli and MurB from Staphylococcus aureus were encouraged for their synthesis. These compounds were synthesized from substituted aromatic Read More

Three- component reactions of 1-(6-hydroxy-2-isopropenyl-1-benzofuran-yl)-1-ethanone, aldehydes and malononitrile or ethyl cyanoacetate in the presence of nanoparticles of ZnO as catalyst are explained as effective and green synthetic method for generating 9H- furo[2,3-f]chromenes in good yield.

Survival of cells and maintenance of genome depend on detection and repair of damaged DNA through intricate mechanisms. Cancer treatment relies on chemotherapy or radiation therapy that kills neoplastic cells by causing immense damage to the DNA. In many cases, escalated DNA repair mechanism leads to resistance against these therapies and therefore, there is a need to expand the interest in developing drugs t Read More

Eighteen hexahydropyrrolo[2,3-b]indole derivatives were synthesized and evaluated their in vitro antifungal activities against five phytopathogenic fungal strains through the mycelium growth rate method. Analysis of the structure-activity relationship on these synthesized compounds revealed that the introduction of benzyl or substituted benzyl group at the C-3a or N-8 position of the pyrroloindoline scaffold conferred higher an Read More

A simple, efficient, and environmentally benign procedure for the synthesis of 2-amino-4Hchromene ring has been achieved by the three-component reaction of an aromatic aldehyde, malononitrile and diverse enolizable C-H activated compound under ultrasound irradiation using sodium carbonate as a catalyst in aqueous media. Sodium carbonate as a natural salt, being available as an inexpensive catalyst combi Read More

A simple and efficient synthesis of pyrimido[b]quinolinetriones is introduced using copper (I) iodide nanoparticles (CuI NPs) as an efficient heterogeneous catalyst in green media-water. The catalyst was prepared through the simple precipitation route and well characterized by various techniques such as XRD and SEM. The mild reaction conditions, using aqueous medium, reusability of the catalyst, simple reaction work- Read More