OBJECTIVES To investigate the potential association between tumour necrosis factor (TNF) inhibitor treatment and malignant melanomas in rheumatoid arthritis, melanoma risks in rheumatoid arthritis patients not treated with biological drugs, and risk of all site cancer with TNF inhibitors as used in rheumatoid arthritis. DESIGN Population based cohort study. SETTING Prospectively recorded da...

A. Al-Hamashi, J. Almaliti, R. Farrell, V. L. Tillekeratne University of Toledo Purpose Histone deacetylase (HDAC) enzymes, which are overexpressed in many cancer tissues, present a potential target for cancer chemotherapy.HDAC inhibitors (HDACis) are currently being investigated as potential anticancer agents. Most of the current HDACis are not selective and have high potential toxicity. Selec...

A series of indolinone-based compounds bearing benzylpyridinium moiety was designed as dual-binding inhibitors of acetylcholinesterase (AChE). The target compounds 3a-u were synthesized by condensation of oxindole and pyridin-4-carbalehyde, and subsequent N-benzylation. The anti-cholinesterase activity evaluation of synthesized compounds revealed that most of them had very potent inhibitory act...

A new series of MMP2 inhibitors is described, following a fragment-based drug design approach. One fragment containing an azide group and a well known hydroxamate Zinc Binding Group in a α-sulfone, α-tetrahydropyrane scaffold, has been synthesized. Water-LOGSY, STD and competition-STD experiments indicate that this fragment binds to the active site of the enzyme. A click chemistry reaction was ...

A series of new thiophene derivatives has been synthesized using the Gewald protocol. The acetylcholinesterase inhibition activity was assayed according to Ellman's method using donepezil as reference. Some of the compounds were found to be more potent inhibitors than the reference. 2-(2-(4-(4-Methoxyphenyl)piperazin-1-yl)acetamido)-4,5,6,7-tetrahydrobenzo[b]thiophene-3-carboxamide (IIId) showe...

Worldwide, cardiovascular disease is considered a major cause of death and disability. Age, sex, blood pressure, total cholesterol, high-density lipoprotein smoking diabetes contribute in the development disease. Hence, cholesterol modulation using cholesteryl ester transfer protein inhibitors could have great role reducing risk mortality. In this work, ten new benzyloxalamides 8a-j were synthe...

In addition to their clinical importance in the treatment of type II diabetes, a-glucosidase inhibitors have attracted considerable attention from the synthetic community because of their profound effect on an array of cellular processes, including N-linked glycoprotein processing and maturation, oligosaccharide metabolism, and cell–cell and cell–virus recognition. Over the past decade, a numbe...

directed at interrupting the inflammatory process, which, if left unchecked, causes irreversible joint damage, deformity and long-term functional impairment. The earlier therapy is initiated, the better the long-term outcomes in patients with RA. Methotrexate is the main disease-modifying anti-rheumatic drug (DMARD) used for the treatment of RA and remains the gold standard of first-line therap...

Reveromycins A, B, C and D showed inhibitory activity against EGF-stimulated mitogen response in Balb/MK cells. Furthermore reveromycins A, C and D exhibited morphological reversion of srcts-NRK cells, antiproliferative activity against human tumor cell lines and antifungal activity. The effects of reveromycins A, C and D on eukaryotic cells were closely similar to each other, but those of reve...