Synthesis and antiproliferative activity of α-branched α,β-unsaturated ketones in human hematological and solid cancer cell lines

Add time:07/15/2019    Source:sciencedirect.com

A series of α-branched α,β-unsaturated ketones were prepared via boron trifluoride etherate mediated reaction between arylalkynes and carboxaldehydes. The evaluation of the antiproliferative activity over hematological (NB4) and solid cancer (A549, MCF-7) cell lines provided a structure-activity relationship. 5-Parameter QSAR equations were built which were able to explain 80%–92% of the variance in activity. The resulting selective lead compound showed IC50 value 0.6 μM against the hematological cell line and did not cause apoptosis, but blocked cell cycle in G0/G1. Moreover, it was demonstrated that this compound enhances and accelerates retinoic acid induced granulocytic differentiation.

We also recommend Trading Suppliers and Manufacturers of CYCLOHEXYL 3-TRIFLUOROMETHYLPHENYL KETONE (cas 3277-77-8). Pls Click Website Link as below: cas 3277-77-8 suppliers

Prev:Further ‘tethered’ Ru(II) catalysts for asymmetric transfer hydrogenation (ATH) of ketones; the use of a benzylic linker and a cyclohexyldiamine ligand
Next:Catalytic hydrogenolysis of aromatic ketones by a sol–gel entrapped combined Pd-[Rh(cod)Cl]2 catalyst)