Hybrid -ionone and curcumin molecules as anticancer agents

Details Hybrid -ionone and curcumin molecules as anticancer agents Hybrid -ionone and curcumin molecules as anticancer agents

C - Chemistry, Metallurgy

07

D

C07D 209/12 (2006.01) A61K 31/12 (2006.01) A61K 31/335 (2006.01) A61K 31/381 (2006.01) A61K 31/403 (2006.01) A61K 31/404 (2006.01) A61K 31/415 (2006.01) A61K 31/47 (2006.01) A61P 35/00 (2006.01) C07C 49/237 (2006.01) C07C 49/255 (2006.01) C07D 209/86 (2006.01) C07D 215/14 (2006.01) C07D 231/06 (2006.01) C07D 333/56 (2006.01)

Patent

CA 2744360

The present invention relates to the synthesis of a series of ionone and curcumin derivatives as multi-targeting agents effective against both hormone-sensitive and hormone-independent cancers. In particular, the present invention is directed to a distinct class of bifunctional antiandrogens, which inhibit both AR and IKBkinases (IKK). A series of ionone-based chalcones were synthesised and their in vitro cytotoxicity against prostate cancer cell lines were demonstrated. A series of derivatives formed by reacting ionone-based chalcones and hydrazines demonstrate substantial antiproliferative activities in prostate cancer, breats cancer and lung cancer cell lines.

La présente invention concerne la synthèse dune série de dérivés dionone et de curcumine en tant quagents de ciblage multiple efficaces contre des cancers hormonosensibles et hormono-indépendants. En particulier, la présente invention concerne une classe distincte dantiandrogènes bifonctionnels, qui inhibent les kinases AR et IKB (IKK). Une série de chalcones à base dionone ont été synthétisées et leur cytotoxicité in vitro contre des lignées cellulaires de cancer de la prostate a été démontrée. Une série de dérivés formés par réaction de chalcones à base dionone et dhydrazines présentent des activités antiprolifératives substantielles dans des lignées cellulaires de cancer de la prostate, de cancer du sein et de cancer du poumon. Formules (I), (II)

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