Synthesis and SAR studies of 5-(pyridin-4-yl)-1,3,4-thiadiazol-2-amine derivatives as potent inhibitors of Bloom helicase.

Journal article

Human cells utilize a variety of complex DNA repair mechanisms in order to combat constant mutagenic and cytotoxic threats from both exogenous and endogenous sources. The RecQ family of DNA helicases, which includes Bloom helicase (BLM), plays an important function in DNA repair by unwinding complementary strands of duplex DNA as well as atypical DNA structures such as Holliday junctions. Mutations of the BLM gene can result in Bloom syndrome, an autosomal recessive disorder associated with c...

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Authors: Rosenthal, A; Dexheimer, T; Gileadi, O; Nguyen, G; Chu, W

• Publication status: Published
• Journal: Bioorganic and medicinal chemistry letters
• Volume: 23
• Issue: 20
• Pages: 5660-5666
• Publication date: 2013-10-01
• DOI: 10.1016/j.bmcl.2013.08.025
• EISSN: 1464-3405
• ISSN: 0960-894X
• Language: English
• Keywords: Enzyme Inhibitors; Humans; Cell Membrane Permeability; Caco-2 Cells; Phenylurea Compounds; Structure-Activity Relationship; Thiadiazoles; RecQ Helicases; Amines