1416725-75-1Relevant academic research and scientific papers
Synthesis and antiproliferative activity of α-branched α,β-unsaturated ketones
Karpaviciene, Ieva,Cikotiene, Inga,Padrón, José M.
, p. 568 - 578 (2013/12/04)
A series of α-branched α,β-unsaturated ketones were prepared in a straightforward manner by the acid catalyzed coupling between arylalkynes and carbaldehydes. The method also allows producing as side product chalcone analogs bearing an additional α,β-unsaturated arylketone in the molecular scaffold. The evaluation of the antiproliferative activity in the human solid tumor cell lines HBL-100 (breast), HeLa (cervix), SW1573 (non-small cell lung), T-47D (breast) and WiDr (colon) provided a structure-activity relationship. Overall, the compounds presented active against the resistant cancer cells T-47D. The resulting lead, displaying an unprecedented chalcone scaffold, showed GI50 values in the range 0.32-0.53 μM against all cell lines tested. The methoxy group present in the lead might play an important role in the activity.
A unique cascade reaction between 3-arylprop-2-inylcarboxylates and benzaldehydes leading to the formation of Morita-Baylis-Hillman adducts
Karpaviciene, Ieva,Cikotiene, Inga
supporting information, p. 224 - 227 (2013/04/24)
During an alkyne-carbonyl metathesis reaction between electron-rich 3-arylprop-2-inylcarboxylates and electron-poor benzaldehydes, a smooth migration of carboxylate groups takes place. This unique cascade reaction allows the formation of Morita-Baylis-Hillman (MBH) adducts unavailable via a traditional MBH reaction.
