Dihydropyrimidine dehydrogenase (DPD) is responsible for degradation of the pyrimidines uracil and thymine and the inactivation of the chemotherapeutic agent 5-fluorouracil. DPD activity is highly variable in cancer populations, and this variation may influence the antitumor efficacy of 5-fluorouracil. However, little is known about the regulation of DPD mRNA expression in any tissues. Using a ...

In the title compound, C(24)H(22)N(2)O(4)S, the central pyrimidine ring is significantly puckered, assuming a conformation inter-mediate between a boat and a screw boat. The nearly planar thia-zole ring (r.m.s. deviation = 0.0258 Å) is fused with the pyriamidine ring, making a dihedral angle of 9.83 (7)°. The carboxyl group is in an extended conformation with an anti-periplanar orientation with...

The mechansim of the three-component Biginelli dihydropyrimidine synthesis was reinvestigated using (1)H and (13)C NMR spectroscopy. Condensation of benzaldehyde, ethyl acetoacetate, and urea (or N-methylurea) in CD(3)OH according to the procedure described by Biginelli produced the expected 6-methyl-2-oxo-4-phenyl-1,2,3,4-tetrahydropyrimidine-5-carboxylates. According to NMR measurements, ther...

Abstract C 14 H 12 N 4 O 3 S, monoclinic, P 2 1 / n (no. 14), a = 12.2777(3) Å, b 9.4312(2) c 12.9412(2) β 107.945(2)°, V 1425.61(5) Å , Z 4, R gt ( F ) 0.0305, wR ref 0.0837, T 160 K.

Adjuvant chemotherapy with 5-fluorouracil remains the basic treatment for patients with advanced colorectal carcinoma. The major obstacle in successful treatment is the ability of CRC cells to acquire chemoresistance. Here we examined the impact of ID1 silencing on the sensitivity of CRC cells to 5-FU. To suppress ID1 expression in HT-29 and HCT-116 cells the cells were transduced with a lentiv...

Dihydropyrimidines 4a-r have been synthesized by base catalysed condensation of beta-aroylpropanoic acid, guanidine nitrate and aromatic aldehyde. Structures of the new compounds were established on the basis of 1H NMR and IR spectral data. Anti-inflammatory activity in vivo was evaluated and compared with standard drug diclofenac sodium.