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Central heterocyclic ring size reduction from piperidinyl to pyrrolidinyl in the vesicular monoamine transporter-2 (VMAT2) inhibitor GZ-793A and its analogs resulted in novel N-propane-1,2(R)-diol analogs 11a-i. These compounds were evaluated for their affinity for the dihydrotetrabenazine (DTBZ) binding site on VMAT2 and for their ability to inhibit… (More)
A series of novel 5-((1-aroyl-1H-indol-3-yl)methylene)-2-thioxodihydropyrimidine-4,6(1H,5H)-diones (3a-z) have been evaluated for in vitro cytotoxicity against a panel of 60 human tumor cell lines. Compound 3k exhibited the most potent growth inhibition against melanoma MDA-MB-435 cells (GI(50)=850 nM), against leukemia SR cancer cells (GI(50)=1.45 μM), and… (More)
In the title compound, C(22)H(28)F(2)NO(2) (+)·CHO(2) (-), there are three independent pyrrolidinium formate salt mol-ecules. In each cation, the central pyrrolidinium ring is not planar and the 2,5-disubstituted phenyl-ethyl groups are in equatorial positions. In the crystal, the ions are linked into a pair of chains parallel to the c axis by N-H⋯O… (More)
In the title compound, C(13)H(13)N(3), the cyano groups at the 2- and 5-positions are eclipsed with each other. The phenyl ring is disordered over two sets of sites, with refined occupancies of 0.520 (5) and 0.480 (5). The angles between the mean plane of the pyrrolidine ring and the two cyano groups are 71.7 (9) and 75.0 (12)°.