The abilities of 7-coumarin propargyl ether (CPE) and 7-(4-trifluoromethyl)coumarin propargyl ether (TFCPE) to act as mechanism-based inactivators of P450 3A4 and 3A5 in the reconstituted system have been investigated using 7-benzyloxy-4-(trifluoromethyl)coumarin (BFC) and testosterone as probes. CPE inhibited the BFC O-debenzylation activity of P450 3A4 in a time-, concentration-, and NADPH-de...

We report on the synthesis of 4-hydroxycoumarin dimers 1-15 bearing an aryl substituent on the central linker and fused benzopyranocoumarin derivatives 16-20 and on their in vitro broad anti-DNA and RNA virus activity evaluations. The chemical identities and structure of compounds 1-20 were deduced from their homo- and heteronuclear NMR measurements whereas the conformational properties of 5, 1...

The polymorphic human cytochrome P450 (P450) 2B6 is primarily responsible for the metabolism of several clinically relevant drugs including bupropion, cyclophosphamide, propofol, and efavirenz. Although a number of single nucleotide polymorphisms have been found in the P450 2B6 gene, the influence of these variants on the metabolism of substrates and on the response to known inactivators of P45...

In the title compound, C(26)H(26)N(2)O(2)S, the dihedral angle between the benzothia-zole and coumarin rings is 8.34 (7)°, indicating that the overall benzothia-zole substituent is almost coplanar with the coumarin rings. An intra-molecular S⋯O [2.813 (1) Å] contact may help to stabilize the mol-ecular conformation. In the crystal structure, π-π stacking inter-actions [centroid-centroid distanc...

In the title compound, 6-benz-yloxy-2H-1-benzopyran-2-one, C(16)H(12)O(3), the coumarin unit and benzyl plane in the mol-ecule are perpendicular to each other [86.92 (7)°]. The crystal packing is stabilized by π-π stacking inter-actions, with an inter-planar separation between inversion-related coumarin units of 3.618 (3) Å. The crystal structure shows inter-molecular C-H⋯O hydrogen bonding bet...

Ti(III),Mn(III) & Co(III) complexes of schiff bases derived from condensation reaction of 3-(2amino-4-thiazolyl)coumarin with 2-hydroxybenzaldehyde,2-hydroxy-3-methoxy benzaldehyde and 2hydroxy-1-napthaldehyde have been prepared and characterised. All the three ligands function as uninegative bidentate coordinating ligands with metal ions through phenolic oxygen and azomethine nitrogen. The com...

On the basis of monitoring the prevention of accumulation of lipid droplets in mouse 3T3-L1 preadipocyte cells and inhibition of the proliferation of human colon cancer HT-29 cells, effective anti-corpulence and anticancer compounds were isolated from the peel of Citrus fruits. These bioactive components were identified as polymethoxyflavones and coumarin derivatives by spectroscopic analyses. ...