Nanoformulated calix[8]arenes functionalized with N-heterocyclic carbene (NHC)-palladium complexes were found to be efficient nano-reactors for Suzuki-Miyaura cross-coupling reactions of water soluble iodo- and bromoaryl compounds with cyclic triol arylborates at low temperature in water without any organic co-solvent. Combined with an improved one-step synthesis of triol arylborates from boronic acid, this remarkably efficient new tool provided a variety of 4′-arylated phenylalanines and tyrosines in good yields at low catalyst loading with a wide functional group tolerance.
Highlights Quinaldinyl-Pyridyl-Indole (QnPyInd) was discovered as novel tubulin inhibitors. Compound 42 displayed excellent antiproliferative activity with average IC 50 of 5.6 nM. 42 exhibited high antiproliferative activity against resistant K562R and HT-29 cell lines. 42 inhibited tubulin polymerization both in vitro and in cells and induced G2/M cell cycle arrest. The safety profile of 42 was demonstrated in human no cancer cells PBLs.
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