What is it about?
Thymidine phosphorylase (TP) overexpression plays a role in several pathological conditions, such as rheumatoid arthritis, chronic inflammatory diseases, psoriasis, and tumour angiogenesis. The inhibitor of this enzyme plays an important role in preventing these threats due to overexpression of TP. In this study, analogues of 3-formylcoumarin were synthesized and screened for thymidine phosphorylase inhibitory activity. Fifteen analogues showed excellent inhibition potential many times better than the standard 7-Deazaxanthine.
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Why is it important?
Angiogenesis is the formation of new blood vessels from pre-existing vessels and is essential for organ growth and repair. However, it is also an important step in cancer growth. Thus, angiogenesis inhibitors are believed to be potential candidates for blocking cancer growth. In particular, TP is a pro-angiogenic factor which catalyzes the reversible phosphorolysis of thymidine into thymine and 20-deoxy-D-ribose 1-phosphate. There is an urgent need to develop new and potent thymidine phosphorylase inhibitors. Coumarins act as intermediates for the synthesis of furocoumarins, chromenes, coumarone, and 2-acylresorcinols. In this paper, the researchers synthesize 3-formylcoumarin analogs and evaluate them for thymidine phosphorylase inhibitory potential.
Perspectives
Coumarin and their derivatives have attracted considerable attention from organic and medicinal chemists over the decades. They are widely used as additives in food, perfumes, agrochemicals, cosmetics, pharmaceuticals and in the preparations of insecticides, optical brightening agents, dispersed fluorescent and tunable laser dye. Coumarin and its derivatives have varied bioactivities such as antimicrobial, antidepressant, antioxidant, anti-inflammatory, antinociceptive, antitumour activities.
Assoc. Prof. Dr. Syed Adnan Ali Shah
Universiti Teknologi MARA
Read the Original
This page is a summary of: Synthesis, molecular docking study and thymidine phosphorylase inhibitory activity of 3-formylcoumarin derivatives, Bioorganic Chemistry, August 2018, Elsevier,
DOI: 10.1016/j.bioorg.2018.02.028.
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