Synthesis and structure–activity relationship of diarylamide derivatives as selective inhibitors of the proliferation of human coronary artery smooth muscle cells

2-Cinnamamido, 2-(3-phenylpropiolamido), and 2-(3-phenylpropanamido)benzamides: Synthesis, antiproliferative activity, and mechanism of action

“…A mixture of 0.01 mol of 6-R-7-R 1 -1 H –benzo[d] [1,3] oxazine-2,4-diones 8b,c and 25 ml of aqueous ammonia solution (25%) was stirred for 1 h. The solid precipitate was removed by filtration, washed with an aqueous ammonia solution (5%) and crystallized from ethanol.…”

“…Some examples of biological activities of this class of compounds include activity against human coronary artery smooth muscle and endothelial cells [1], antifibrotic and antiinflammatory properties [2,3], inhibition of cornea pterygium progression and blood vessel development [4,5] and prevention and treatment of renal glomerular diseases [6]. In a previous paper from our laboratories [7], we reported the synthesis, antiproliferative activity and mechanism of action of a series of 2-{[2 E ]-3-phenylpropenamido}benzamides 1a–v (Fig.…”

Synthesis, antiproliferative activity, and mechanism of action of a series of 2-{[(2E)-3-phenylprop-2-enoyl]amino}benzamides

“…Tranilast (Rizaben ® ) 2 is an antiallergic drug approved in 1982 for use in Japan and South Korea for bronchial asthma and was also investigated for use as an antiproliferative agent on drug-eluting stents. Its derivative ( E )-2-(3-(3,4-dime-thoxyphenyl)acrylamido)benzamide 3 [1] is another member of this class of compounds and is more potent than the lead compound, Tranilast (Fig. 1).…”

Synthesis, antiproliferative activity and possible mechanism of action of novel 2-acetamidobenzamides bearing the 2-phenoxy functionality

“…Despite their wide range of biological activities, 1–6 a review of the literature revealed that no anticancer activity had been described for these compounds. This omission led us to explore the potential of this class of compounds as anticancer agents by synthesizing and screening for antileukemic activity a series of novel 2-cinnamamido, 2-(3-phenylpropiolamido) and 2-(3-phenylpropanamido)benzamides.…”