3033099-32-7
Chemical Structure
Tubulin Polymerization-IN-1 prodrug
- CAS No.: 3033099-32-7
- Formula:C22H23FN2O4
- Molecular Weight:398.43
InChIKey: QOPRLCWEGYCGLP-UHFFFAOYSA-N
SMILES: FC(C=C1C(NCC2=CC=C(OC)C(OCC#C)=C2)=O)=CC=C1N3CCOCC3
Biological Activity: Tubulin Polymerization-IN-1 prodrug (Compound 2b) is a palladium (Pd)-mediated tubulin polymerization inhibitor prodrug. Developed based on colchicine binding site inhibitors (CBSIs), it reduces toxicity and enhances targeted release properties. Compared to the parent compound, Tubulin Polymerization-IN-1 prodrug exhibited 68.3-fold lower cytotoxicity, which can be restored in situ in the presence of Pd resin. Mechanistic studies showed that its anticancer activity is consistent with CBSIs. In vivo, Tubulin Polymerization-IN-1 prodrug significantly inhibited tumor growth (63.2%) when activated by Pd resin. It holds promise for research in the field of anticancer therapy[1].
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Tubulin Polymerization-IN-1 prodrug | Tubulin Polymerization-IN-1 prodrug (Compound 2b) is a palladium (Pd)-mediated tubulin polymerization inhibitor prodrug. Developed based on colchicine binding site inhibitors (CBSIs), it reduces toxicity and enhances targeted release properties. Compared to the parent compound, Tubulin Polymerization-IN-1 prodrug exhibited 68.3-fold lower cytotoxicity, which can be restored in situ in the presence of Pd resin. Mechanistic studies showed that its anticancer activity is consistent with CBSIs. In vivo, Tubulin Polymerization-IN-1 prodrug significantly inhibited tumor growth (63.2%) when activated by Pd resin. It holds promise for research in the field of anticancer therapy. | |||||||||||||||||||||
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Keywords
