Yu, Han; Dai, Guoyong; He, Qiu-Rui; Tang, Jiang-Jiang published the artcile< Enantioselective synthesis and evaluation of 4-styryldihydropyrimidin-2-thiones as anti-proliferative agents>, Reference of 3893-18-3, the main research area is styryldihydropyrimidinethione preparation enantioselective anticancer; cinnamaldehyde thiourea ketoester Biginelli reaction organocatalyst.
A series of novel chiral (S)-4-styryldihydropyrimidin-2-thiones I (R1 = H, F, NO2, etc.; R2 = i-Pr, t-Bu; R3 = Me, Et) was prepared with high yields and enantioselective by a Biginelli reaction. In the condensation reaction, substituted cinnamaldehyde R1C6H4CH=CHCHO, thiourea and β-ketoesters R2C(O)CH2C(O)2R3 were organocatalyzed to afford 4-styryldihydropyrimidin-2-thiones I using self-assembled methanoproline-thiourea as catalysts. Anti-proliferative activity of these 4-styryldihydropyrimidin-2-thiones I was tested against the HepG2 and PC-3 cells. Among all the tested compounds, I (R1 = CF3; R2 = i-Pr, t-Bu; R3 = Me, Et) bearing CF3- groups at styryl group displayed a moderate anti-proliferative activity with IC50 ranged between 29.3-38.5 μM. The structure-activity relationship showed that substituents (R1) on the C-4 styryl ring of 4-styryldihydropyrimidin-2-thiones and R3 at ester group affected the anti-proliferative activity, yet R2 at C-6 position had little influence for anti-proliferative activity.
Medicinal Chemistry Research published new progress about Antitumor agents. 3893-18-3 belongs to class bromides-buliding-blocks, and the molecular formula is C9H7BrO, Reference of 3893-18-3.
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary