Design, synthesis and antitumor activities of oxazolo[5, 4-d] pyrimidine derivatives / 中国药科大学学报

A series of oxazole[5,4-d] pyrimidine derivatives were designed and synthesized to discover novel compounds with antitumor activity.Compounds 8a-8m were synthesized using acetamidine hydrochloride as the start material.The structures of synthesized compounds were confirmed by IR,1H NMR,EI-MS and elemental analysis.The antiangiogenesis activities of the synthesized compounds were determined by MTT in human umbilical vein endothelial cell (HUVEC).The in vitro antitumor activities of the synthesized compounds were determined by MTT assay in A549,HepG2 and U251.Compounds 8c,8d,8g,8i and 8l were found to inhibit the proliferation of all the tested cell lines.Compound 8l exhibited noteworthy activities in A549,HepG2 and U251 cell lines with IC50value lower than the positive reference sunitinib,suggesting that compound 8l might be the promising antitumor agent for further investigation.

Pyrimidinethione derivatives with tosyl substitution: Synthesis, and antimicrobial property investigation.

Substitution of tosyl group on hydroxyacetophenones orhydroxybenzaldehyde and their subsequent condensation yielded several tosyloxy substituted chalcones which were derivatized to obtain the corresponding pyrimidinethione derivatives. The synthesized compounds were characterized by spectroscopic techniques like FT-IR, 1H NMR, 13C NMR, and mass spectrometry. These compounds were subjected to initial screening for their bioactivity using zone of inhibition method and were found moderately active against the tested microorganisms, viz. Mycobacterium smegmatis, Staphylococcus aureus, Escherichia coli, and Candida albicans.

Synthesis and antitumor activities of 8-aminobenzofuran3, 2-d pyrimidine derivatives / 中国药学杂志

OBJECTIVE: To synthesize the derivatives of 8-amino benzofuran[3, 2-d] pyrimidine and study their anticancer activiies. METHODS: The target compounds were synthesized through a series of reactions, and their anticancer activities in vitro were evaluated against COLO205, MCF-7 and K562 cell lines by MTT as assay. RESULTS: Nine title compounds were synthesized and confirmed by EI-MS, 1H-NMR and 13C-NMR. Compounds 2, 3d and 5c had good inhibition effect against COLO205, MCF-7 and K562 cells. The inhibition rates of compound 5c against COLO205, MCF-7 and K562 cells were 99.58%, 78.75% and 98.68% respectively at 10-4 mol · L-1. CONCLUSION: The anticancer activity of benzofuran[3, 2-d] pyrimidine derivatives is worthy of further study.