Synthesis and biological evaluation of a new series of N-ylides as protein farnesyltransferase inhibitors
A new family of 30 benzoylated N-ylides 4 and 5 was synthesized and evaluated for the inhibitory activity on human protein farnesyltransferase. Most of these novel compounds possessed in vitro inhibition potencies in the micromolar range. The nature of th
Abuhaie, Cristina-Maria,Ghinet, Alina,Farce, Amaury,Dubois, Jo?lle,Rigo, Beno?t,B?cu, Elena
Synthesis and biological evaluation of a new series of phenothiazine- containing protein farnesyltransferase inhibitors
Two new families of human farnesyltransferase inhibitors 13a-m and 14a-d, based on a phenothiazine scaffold, were synthesized. Compounds 14a and 14b were the most promising inhibitors of human farnesyltransferase with IC50 values of 0.7 and 0.6 μM, respectively.
Abuhaie, Cristina-Maria,Ghinet, Alina,Farce, Amaury,Dubois, Joelle,Gautret, Philippe,Rigo, Benoit,Belei, Dalila,Bicu, Elena
p. 101 - 110
(2013/03/13)
Oral Hypoglycemic Agents. Discovery and Structure-Activity Relationships of Phenacylimidazolium Halides
Blood glucose levels in viable, yellow, obese, diabetic mice are reduced following oral administration of phenacylimidazolium halides.Compounds 2 and 3 produced reductions of ca. 40percent 2 h after doses of 100 mg/kg po.Since these mice do not respond to sulfonylureas, the glucose-lowering activity of phenacylimidazolium salts in this model suggests a mechanism other than that of stimulating insulin secretion.Only phenacylimidazolium halides with electron-donating groups were active; other azolium salts or variations in the phenacyl portion (alterations in the keto function; chain lengthening or extensive branching) produced inactive compounds.
Dominianni, Samuel J.,Yen, Terence T.
p. 2301 - 2306
(2007/10/02)
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