annulation between 2-aminobiphenyls and activated olefins is disclosed for succinct synthesis of valuable phenanthridine scaffolds. The protocol avails a common organic functional group, free amine, as a directing group and represents a unique combination of C–Hactivation/annulation/C–C bond cleavage cascade that bodes well in the production of bioactive alkaloids including trisphaeridine and bicolorine
series of N-sulfonyl-aminobiaryl derivatives have been examined as novel antitubulinagents. Compound 21 [N-(4′-cyano-3′-fluoro-biphenyl-2-yl)-4-methoxy-benzenesulfonamide] exhibits remarkable antiproliferative activity against four cancer cell lines (pancreatic AsPC-1, lung A549, liver Hep3B, and prostate PC-3) with a mean GI50 value of 57.5 nM. Additional assays reveal that 21 inhibits not only tubulin
Compounds of formula I are provided
1
as well as pharmaceutically acceptable salts and esters thereof, wherein R
1
to R
8
and n have the significance given in the specification can be used to treat non-insulin dependent diabetes mellitus.
An efficient synthesis of free (NH)-phenanthridinones through Pd-catalyzed C(sp(2))-H aminocarbonylation of unprotected o-arylanilines under an atmospheric pressure of CO has been developed. Some ortho heteroarene substituted anilines as well as N-alkyl protected o-arylanilines are also suitable substrates for this C-H aminocarbonylation reaction.
The invention relates to acid halide and/or acyllactam functional compounds, to polylactam block copolymers derived therefrom by lactam polymerization at a lactam group, and to the use of such block copolymers in polyamide mixtures. The compounds contain liquid crystalline compounds or compounds which combine with acyllactam to form a compound with liquid crystalline properties. The products of this invention are useful as accelerators in the preparation of nylon block copolymers, in particular block copolymers with improved stiffness. The block copolymers are useful in products requiring good tensile strength, chemical resistance and/or heat resistance, and are particularly useful in electrical engineering applications and in the aircraft industry.