SYNTHESIS OF NOVEL TUBULIN POLYMERIZATION INHIBITORS: BENZOYLPHENYLUREA (BPU) SULFUR ANALOGS

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United States of America Patent

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12471585

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A novel series of BPU analogues were synthesized and evaluated for antitumor activity. In particular, BPU sulfur analogues 6n and 7d were shown to possess up to 10-fold increased potency, when compared to compound 1, against cancer cell lines. 6n was more effective than compound 1 in causing apoptosis of MCF-7 cells. When compared to other drugs with a similar mechanism of action, 6n retained significant ability to inhibit tubulin assembly, with an IC50 of 2.1 μM.

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CHAMPIONS BIOTECHNOLOGY INC855 NORTH WOLFE STREET BALTIMORE MD 21205

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Inventor Name Address # of filed Patents Total Citations
Hallur, Gurulingappa Owlings Mills, US 16 40
Hidalgo, Manuel Baltimore, US 69 323
Jimeno, Antonio Englewood, US 11 40
Khan, Saeed R Owlings Mills, US 9 39

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