Targeting Cancer Stem Cells with Novel 4-(4-2 substituted phenyl)-5-(3,4,5-trimethoxy/3,4-dimethoxy)-3 benzoyl-3,4-dihydropyrimidine-2(1H)-one/thiones.

Journal Article

Al-Omar, Mashooq A. Bhat, Abdullah Al-Dhfyan, Mohamed A. . 2016

• نوع عمل المنشور: patent
• الوسوم: cancer stem cell
• المجلة \ الصحيفة: Molecules
• رقم الإصدار السنوي: 21
• الصفحات: 1746-1755

مستخلص المنشور

Novel 4-(4-substituted phenyl)-5-(3,4,5-trimethoxy/3,4-dimethoxy)-benzoyl-3,4-
dihydropyrimidine-2(1H)-one/thione derivatives (DHP 1–9) were designed, synthesized,
characterized and evaluated for antitumor activity against cancer stem cells. The compounds were
synthesized in one pot. Enaminones E1 and E2 were reacted with substituted benzaldehydes and
urea/thiourea in the presence of glacial acetic acid. The synthesized compounds were characterized
by spectral analysis. The compounds were screened in vitro against colon cancer cell line (LOVO)
colon cancer stem cells. Most of the compounds were found to be active against side population
cancer stem cells with an inhibition of >50% at a 10 M concentration. Compounds DHP-1, DHP-7
and DHP-9 were found to be inactive. Compound DHP-5 exhibited an in vitro anti-proliferative
effect and arrested cancer cells at the Gap 2 phase (G2) checkpoint and demonstrated an inhibitory
effect on tumor growth for a LOVO xenograft in a nude mouse experiment