The present study reports the synthesis, structural characterization and
myorelaxant activity evaluation of a series of 16 novel
4-naphthyl-hexahydroquinoline derivatives. The compounds were achieved by
one-pot microwave-assisted method via a modified Hantzsch reaction. The
structures of the compounds were confirmed by various spectral methods like
IR, 1D-2D NMR techniques and mass analysis. X-ray studies of compound 10
provided further evidence for the proposed structure. To evaluate their
myorelaxant activities, the Emax and pD2 values of the compounds and
nifedipine were determined on isolated rabbit gastric fundus smooth muscle
strips. The obtained results indicated that introduction of long chain alkyl
groups such as 2-methoxyethyl or 2-(methacryloyloxy)ethyl moiety to the ester
group led to the most active compounds.
A series of 1-8 different ferrocenyl chalcones were synthesized through the Claisen-Schmidt condensation and the Friedel−Crafts acylation. Their structures were confirmed by means of 1 H, 13 C NMR and FT−IR. The cytotoxic and antiproliferative activities of the chalcones were screened against HeLa (cervix cancer) and PC3 (prostate cancer) cell lines. They showed excellent anticancer activities especially against PC3 cell even at very low concentration (5 µM). Also, their physicochemical properties, drug-likeness calculations and the rule of five (RO5) were investigated.
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