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Title: Synthesis and evaluation of effective photoaffinity probe molecule of furospinosulin-1, a hypoxia-selective growth inhibitor. Author: Kotoku N, Nakata C, Kawachi T, Sato T, Guo XH, Ito A, Sumii Y, Arai M, Kobayashi M. Journal: Bioorg Med Chem; 2014 Apr 01; 22(7):2102-12. PubMed ID: 24631363. Abstract: The synthesis and evaluation of a photoaffinity probe molecule for furospinosulin-1, a hypoxia-selective growth inhibitor that we identified from marine sponge, was studied. An analogue carrying an alkyne tail showed potent hypoxia-selective inhibitory activity exceeding that of the parent molecule, and exhibited in vivo anti-tumor activity following oral administration. The alkyne moiety in the analogue was also found to be a good anchoring group for the preparation of probe molecules; a photoaffinity probe molecule having an optimized spacer length was selected through the systematic synthesis of several probes and the evaluation of their hypoxia-selective growth inhibitory activity and electrophoretic mobility shift properties.[Abstract] [Full Text] [Related] [New Search]