Lai, Kuo-Chu; Chia, Yi-Ting; Yih, Ling-Huei; Lu, Yi-Liang; Chang, Shih-Ting; Hong, Zi-Xuan; Chen, Tai-Lin; Hour, Mann-Jen published the artcile< Antitumor effects of the novel quinazolinone Holu-12: induction of mitotic arrest and apoptosis in human oral squamous cell carcinoma CAL27 cells>, Name: 2-Amino-4,5-dimethoxybenzamide, the main research area is quinazolinone mitotic arrest human oral squamous cell carcinoma apoptosis; 5-FU sensitivity; Quinazolinone derivatives; apoptosis; human oral squamous cell carcinoma; mitotic arrest.
Quinazolinone is a privileged chem. structure employed for targeting various types of cancer. This study aimed to demonstrate the antitumor activity of synthesized 6,7-disubstituted-2-(3-fluorophenyl) quinazolines (HoLu-11 to HoLu-14). The cytotoxicity was assessed by the sulforhodamine B (SRB) assay. The cell cycle was examined by flow cytometry. The expression levels of cell cycle- and apoptosis-related proteins were estimated by western blotting. A xenograft animal model was used to explore the antitumor effects of HoLu-12. Among four synthetic quinazolinone derivatives, HoLu-12 significantly reduced the viability of oral squamous cell carcinoma (OSCC) cells. HoLu-12 induced G2/M arrest and increased the expression of cyclin B, histone H3 (Ser10) phosphorylation, and cleaved PARP, indicating that HoLu-12 could induce mitotic arrest and then apoptosis. Moreover, the combination of HoLu-12 and 5-fluorouracil (5-FU) displayed synergistic toxic effect on OSCC cells. HoLu-12 significantly inhibited tumor growth in vivo. HoLu-12 induces mitotic arrest and leads to apoptosis of OSCC cells. Furthermore, HoLu-12 alone or in combination with 5-FU is a potential therapeutic agent for OSCC.
Anticancer Research published new progress about Antitumor agents. 5004-88-6 belongs to class amides-buliding-blocks, and the molecular formula is C9H12N2O3, Name: 2-Amino-4,5-dimethoxybenzamide.
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Amide – an overview | ScienceDirect Topics