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Recently Published Articles
- Design, Synthesis, and Local Anti-Inflammatory Activity of 17β-Carboxamide Derivatives of Glucocorticoids
Vladimir Dobričić, Bojan Marković, Nikola Milenković, Vladimir Savić, Vesna Jaćević, Nemanja Rančić, Sote Vladimirov and Olivera Čudina
Article first published online: 27 AUG 2014 | DOI: 10.1002/ardp.201400165
The combination of molecular docking studies and the exponential model for glucocorticoid receptor binding affinity prediction was used for the selection of 17β-carboxamide steroids with potential local anti-inflammatory activity. Local anti-inflammatory activity test and additional in vivo and in silico experiments indicate that these derivatives might be new soft glucocorticoids with significantly better biological profile than dexamethasone.
- Rationally Designed Less Toxic SPD-304 Analogs and Preliminary Evaluation of Their TNF Inhibitory Effects
Polyxeni Alexiou, Athanasios Papakyriakou, Evangelos Ntougkos, Christos P. Papaneophytou, Fotini Liepouri, Anthi Mettou, Ioannis Katsoulis, Anna Maranti, Katerina Tsiliouka, Alexandros Strongilos, Sotiria Chaitidou, Eleni Douni, George Kontopidis, George Kollias, Elias Couladouros and Elias Eliopoulos
Article first published online: 27 AUG 2014 | DOI: 10.1002/ardp.201400198
A series of SPD-304 analogs was rationally designed aiming to diminish its toxicophore groups while maintaining its tumor necrosis factor alpha (TNF) inhibitory activity. Modification of the N-indole substituent with an aromatic deactivating group, in combination with elimination of the 6′-methyl group of the 4-chromone of SPD-304, resulted in a significantly less toxic and equally potent TNF inhibitor (3c).
- An Elegant Microwave Assisted One-Pot Synthesis of Di(α-aminophosphonate) Pesticides
Gangireddy Chandra Sekhar Reddy, Chinthaparthi Radha Rani, Mudumala Veera Narayana Reddy and Cirandur Suresh Reddy
Article first published online: 21 AUG 2014 | DOI: 10.1002/ardp.201400213
New di(α-aminophosphonate) derivatives with pesticidal activity were prepared by Kabachnik–Fields reaction under solvent- and catalyst-free conditions using microwave irradiation. Among all the compounds, 4f, 4c, and 4h exhibited good activity against Spodoptera litura, with 92.6, 91.3, and 89.3% mortality.
- Synthesis and Biological Evaluation of Glucosyl Curcuminoids
Adari Bhaskar Rao, Ernala Prasad, Seelam S. Deepthi and Imtiaz A. Ansari
Article first published online: 20 AUG 2014 | DOI: 10.1002/ardp.201400195
Although curcuminoids possess a wide spectrum of antitumor properties, they have so far not been clinically used to treat cancer, due to their low bioavailability in humans. Glucosylation of curcumin increases its solubility and leads to enhanced anticancer activity. Tetrahydrocurcumin-4,4-β-di-glucoside (glucosyl-THC) showed enhanced free radical scavenging and tyrosinase inhibition activity, improving its medical value.
- 1-Acetyl-3,5-diaryl-4,5-dihydro(1H)pyrazoles: Exhibiting Anticancer Activity through Intracellular ROS Scavenging and the Mitochondria-Dependent Death Pathway
Jimi M. Alex, Sandeep Singh and Raj Kumar
Article first published online: 19 AUG 2014 | DOI: 10.1002/ardp.201400199
Analogs of 1-acetyl-4,5-dihydro(1H)pyrazoles (JP-1–17) were synthesized and evaluated for their anti-proliferative activity in four cancer cell lines and for their intracellular ROS scavenging properties. An attempt was made to determine the mitochondrial membrane potential of MCF-7 cells treated with JP-1 and -14, aiming to elucidate the mechanism by which proliferation was curbed.