C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 211/44 (2006.01) A61K 31/45 (2006.01) A61P 35/00 (2006.01)
Patent
CA 2630465
The present invention relates to 4-piperidone derivatives represented by the following formula (I) and the acid addition salts thereof. The method of preparation and antineoplastic activity of the said compounds are disclosed. A number of the compounds possess submicromolar IC50 and CC50 values and have a selective toxicity for colon cancers and leukemic cells. In addition, many of the compounds are able to reverse multidrug resistance.
La présente invention concerne des dérivés de 4-pipéridone de formule (I) suivante ainsi que les sels d'addition acide desdits dérivés. La présente invention porte également sur la méthode de synthèse et l'activité antinéoplasique desdits composés. Plusieurs des composés selon l'invention présentent des valeurs de CI50 et de CC50 inférieures à la micromole par litre, ainsi qu'une toxicité sélective vis-à-vis des cancers du côlon et des cellules leucémiques. En outre, plusieurs des composés sont susceptibles d'inverser la résistance pléïotrope.
Das Umashankar
Dimmock Jonathan R.
Borden Ladner Gervais Llp
University Of Saskatchewan
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