AI Article Synopsis
- A new photoaffinity probe molecule for furospinosulin-1, a compound from marine sponge that inhibits growth in low oxygen conditions, was developed and evaluated.
- An analogue featuring an alkyne tail demonstrated greater hypoxia-selective inhibitory effects and showed promise against tumors when administered orally.
- The alkyne component was effective for creating probe molecules, and researchers optimized the spacer length in the probes through systematic testing for enhanced growth inhibition and mobility characteristics.
Article 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.
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| http://dx.doi.org/10.1016/j.bmc.2014.02.026 | DOI Listing |
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