4 research outputs found
CCDC 827537: Experimental Crystal Structure Determination
An entry from the Cambridge Structural Database, the worlds repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available from the CCDC and typically includes 3D coordinates, cell parameters, space group, experimental conditions and quality measures
Selenopheno[3,2-<i>c</i>]- and [2,3-<i>c</i>]coumarins: Synthesis, cytotoxicity, angiogenesis inhibition, and antioxidant properties
Synthesis and Studies of Calcium Channel Blocking and Antioxidant Activities of Novel 4-Pyridinium and/or N-Propargyl Substituted 1,4-Dihydropyridine Derivatives
The novel 1,4-DHP derivatives containing the cationic pyridine moiety at the position 4, and the N-propargyl group as a substituent at position 1 of the 1,4-DHP cycle were designed, synthesised, and assessed in biological tests
Synthesis and studies of calcium channel blocking and antioxidant activities of novel 4-pyridinium and/or N-propargyl substituted 1,4-dihydropyridine derivatives
The novel 1,4-dihydropyridine derivatives containing the cationic pyridine moiety at the
position 4, and the N-propargyl group as a substituent at position 1 of the 1,4-DHP cycle
were designed, synthesised, and assessed in biological tests. Among all the novel
compounds, the 4-(N-dodecyl) pyridinium group-containing compounds 11 (without the
N-propargyl group) and 12 (with the N-propargyl group) demonstrated the highest
calcium antagonistic properties against neuroblastoma SH-SY5Y (IC50 about 5–14 mM)
and the vascular smooth muscle A7r5 cell (IC50 – 0.6–0.7 mM) lines, indicating that they
predominantly target the L-type calcium channels. These compounds showed a slight total
antioxidant activity. At concentrations close to those of L-type calcium channel blocking
ones, compound 12 did not affect mitochondrial functioning; also, no toxicity was
obtained in vivo. The N-propargyl group as a substituent at position 1 of the 1,4-DHP cycle
did not essentially influence the compounds’ activity. The 4-(N-dodecyl) pyridinium
moiety-containing compounds can be considered as prototype molecules for further
chemical modifications and studies as cardioprotective/neuroprotective agents.This study was supported by ESF project No. 2009/
0217/1DP/1.1.1.2.0/09/APIA/VIAA/031; the EuroNanoMed
project ‘‘CheTherDel’’; Portuguese Research Council
(FCT), Faculty of Medicine, Centre for Neuroscience and
Cell Biology (CNC) and Marine and Environmental
Research Centre (IMAR–CMA) of the University of
Coimbra, Portugal