- Optical Resolution and Circular Dichroism Spectra of Mixed-diamine Palladium(II) Complexes with Configurational Chirality
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Six square-planar complexes, (ClO4)2 (meso-stien = meso-1,2-diphenyl-1,2-ethanediamine; L = N,N-diethylethylenediamine, N,N-dimethylethylenediamine, 2-methyl-1,2-propanediamine, N2,N2-dimethyl-2-methyl-1,2-propanediamine, N,N-dimethyl-1,3-propenediamine, and (2S)-N1,N1-diethyl-1,2-propanediamine), were prepared and optically resolved (or separated in the case of the last named ligand) using diacetyl-d-tartaric anhydride as the resolving agent.Their electronic absorption and CD spectra were measured.A definite additivity has been confirmed between the configurational CD caused by the chiral configuration and the vicinal CD due to the asymmetric carbon atom in the (2S)-N1,N1-diethyl-1,2-propanediamine complex.Absolute configurations of this and the other five complexes have been assigned by examining molecular models and the CD spectra.
- Nakayama, Kazuhiko,Komorita, Takashi,Shimura, Yoichi
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- METHYLENEDIOXYBENZO [I] PHENANTHRIDINE DERIVATIVES USED TO TREAT CANCER
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The invention provides compounds of formula I: wherein A, B, X, and Y have any of the values defined in the specification, as well as pharmaceutical compositions comprising such compounds, processes for preparing such compounds, and therapeutic methods fo
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Page/Page column 21-22
(2010/09/18)
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- Thiazole benzamide derivatives and pharmaceutical compositions for inhibiting cell proliferation, and methods for their use
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Aminothiazole compounds with mono-/di-substituted benzamide are represented by the Formula (I), and their pharmaceutically acceptable salts, pharmaceutically acceptable prodrugs, pharmaceutically active metabolites, and pharmaceutically acceptable salts of said metabolites are described. These agents modulate and/or inhibit the cell proliferation and activity of protein kinases and are useful as pharmaceuticals for treating malignancies and other disorders.
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- Serotoninergic properties of new conformationally restricted benzamides
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A new series of benzamides derived from metoclopramide have been synthesized, in which the vicinal carbon of the basic nitrogen atom of the ethyl chain is situated on the C3, C4, C5 and C6 rings. The diamino derivatives were prepared through Strecker's reaction from the corresponding ketones except for the cyclopropyl derivatives where 1-ethoxy-1-trimethylsiloxy cyclopropane was used as the starting material. The benzamides were prepared using the mixed anhydride method. They were tested in binding assays for D2, 5-HT3 and 5-HT4 receptors. The results show a marked increase in the selectivity and potency of these derivatives for 5-HT3 receptors with regard to metoclopramide (compound 1d: 5-HT3 K(i) = 9.03 nM; 5-HT4 K(i) > 5000; D2 K(i) > 5000). The influences of steric hindrance and hydrophobic properties on the affinity of benzamide derivatives for 5-HT3 receptors were also emphasized by these data. The X-ray crystal structure of compound 1d was compared with that of the minimal energy conformer of BRL 24682, a reference 5-HT3 receptor antagonist benzamide, determined using the Random Search program. Superimposition of the two structures showed a suitable fit between the pharmacophore groups previously determined to be important for 5-HT3 receptor antagonists. On the other hand, the hydrophobic parts of the basic moieties had different spatial occupancies.
- Yang,Bremont,Shen,Kefi,Langlois
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p. 231 - 239
(2007/10/03)
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