The title compound, C20H17F3N2O4, named tasquinimod, is a second-generation oral quinoline-3-carboxamide analogue, which is currently in phase III clinical trials for the treatment of metastatic prostate cancer. The quinoline unit is almost planar (r.m.s. deviation of fitted atoms = 0.0075 Å). The carboxamide side chain, substituted at position 3, is tilted by 88.07 (7)° to the quinoline plane....

As a part of ongoing studies in developing new anticancer agents, novel 1,2-dihydropyridine 4, thienopyridine 5, isoquinolines 6-20, acrylamide 21, thiazolidine 22, thiazoles 23-29 and thiophenes 33-35 bearing a biologically active quinoline nucleus were synthesized. The structure of newly synthesized compounds was confirmed on the basis of elemental analyses and spectral data. All the newly sy...

Four copper(II) complexes and one copper(I) complex with pyridine-containing pyridylalkylamide ligands N-(pyridin-2-ylmethyl)pyrazine-2-carboxamide (HL) and N-(2-(pyridin-2-yl)ethyl)pyrazine2-carboxamide (HL) were synthesized and characterized. The X-ray crystal structures of [Cu2(L )2(4,4ʹ-bipy)(OTf )2] (1, OTf = trifluoromethanesulfonate, 4,4ʹ-bipy = 4,4ʹ-bipyridine) and [Cu(L)(py)2]OTf·H2O (...

The mol-ecular conformation of the title compound, C(20)H(29)N(3)O(2), is stabilized by an intra-molecular C-H⋯O hydrogen bond. The orientation of the amide group to the ring system is characterized by a C-C-C-O dihedral angle of 137.5 (3)°. In the crystal, inter-molecular N-H⋯O hydrogen bonds between the amide groups form C(4) chains running parallel to the a axis.

In the title compound, C(25)H(24)N(2)O(2), the dihedral angle between the two benzene rings of the benzophenone moiety is 59.10 (6)°. An intra-molecular, bifurcated N-H⋯(O,N) hydrogen bond, which generates S(6) and S(5) rings, respectively, helps to establish the overall conformation of the mol-ecule.

In the title mol-ecule, C(25)H(19)NO(2), the furyl ring is twisted by 46.3 (1)° with respect to the phenyl-ene ring bearing the amido group. In the stilbene unit, the two phenyl-ene rings (i.e. the rings connected through the -CH=CH- fragment) are twisted by 59.2 (1)°; in the biphenyl-ene unit, the two benzene rings are twisted by 35.5 (1)°. In the crystal structure, mol-ecules are linked by an...

A series of twelve amides was synthesized via aminolysis of substituted pyrazinecarboxylic acid chlorides with substituted benzylamines. Compounds were characterized with analytical data and assayed in vitro for their antimycobacterial, antifungal, antibacterial and photosynthesis-inhibiting activity. 5-tert-Butyl-6-chloro-N-(4-methoxybenzyl)pyrazine-2-carboxamide (12) has shown the highest ant...