4.7 Article

Synthesis and biological evaluation of 1,2-dithiol-3-thiones and pyrrolo[1,2-a]pyrazines as novel hypoxia inducible factor-1 (HIF-1) inhibitor

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BIOORGANIC & MEDICINAL CHEMISTRY
卷 24, 期 12, 页码 2843-2851

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PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2016.04.054

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Hypoxia inducible factor-1; VEGF; GLUT-1; Oltipraz; Pyrrolopyrazine

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Hypoxia-inducible factor-1 (HIF-1) is a key transcription factor which is strongly associated with tumor survival, progression, and therapeutic resistance. Accordingly, it has been suggested that the inhibition of the HIF-1 pathway can suppress tumor, and it has become an important therapeutic target. In present study, oltipraz, its metabolite M2, and their derivatives were synthesized and evaluated as HIF-1 alpha inhibitors. Among the synthesized, benzyl-substituted pyrrolo[1,2-a]pyrazine 2g most potently inhibited HIF-1 alpha protein accumulation (81% at 10 mu M) and VEGF, GLUT-1 transcription (77% and 92% at 10 mu M, respectively). (C) 2016 Elsevier Ltd. All rights reserved.

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