Synthesis and Biological Evaluation of Phthalazinone Inhibitors of ...
Synthesis and Biological Evaluation of Phthalazinone Inhibitors of ...
Synthesis and Biological Evaluation of Phthalazinone Inhibitors of ...
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Results <strong>and</strong> Discussion<br />
Scheme I. General Procedure for the <strong>Synthesis</strong> <strong>of</strong> Amide Derivatives.<br />
Reagents <strong>and</strong> Conditions : a) Ph3PCHCO2Et, CHCl3, reflux, 16 h. b) NH2-NH2 or<br />
NH2-NHMe, EtOH, reflux, 3 h. c) 3M NaOH/THF, reflux, 2 h followed by<br />
acidification. d) R’-NH2, EDC, HOBt, DIPEA, DMSO, 3-5 h.<br />
Table I. Initial lead optimization/IC50 values for Acyclic analogs.<br />
Cmpd R R’ (-)-BSA (nM) (+)-BSA (nM)<br />
D1 7 Me 4-OMePh 1000 ± 250 970 ± 250<br />
D20 8 Me 3-OMePh >5000 ND<br />
4
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