Anh, Duong T.; Hai, Pham-The; Huy, Le D.; Ngoc, Hoang B.; Ngoc, Trinh T. M.; Dung, Do T. M.; Park, Eun J.; Song, In K.; Kang, Jong S.; Kwon, Joo-Hee; Tung, Truong T.; Han, Sang-Bae; Nam, Nguyen-Hai published the artcile< Novel 4-Oxoquinazoline-Based N-Hydroxypropenamides as Histone Deacetylase Inhibitors: Design, Synthesis, and Biological Evaluation>, Category: bromides-buliding-blocks, the main research area is oxoquinazoline hydroxypropenamide preparation histone deacetylase inhibitor antitumor mol docking.
Two series of novel 4-oxoquinazoline-based N-hydroxypropenamides I (R = Et, Bn, 4-FC6H5, etc.) and II were designed, synthesized, and evaluated for their inhibitory and cytotoxicity activities against histone deacetylase (HDAC). The compounds showed good to potent HDAC inhibitory activity and cytotoxicity against three human cancer cell lines (SW620, colon; PC-3, prostate; NCI-H23, lung cancer). In this series, compounds with the N-hydroxypropenamide functionality impeded at position 7 on the 4-oxoquinazoline skeleton II were generally more potent than compounds I with the N-hydroxypropenamide moiety at position 6. Also, the N3-benzyl-substituted derivatives exhibited stronger bioactivity than the N3-alkyl-substituted ones. Two compounds II (R = 4-ClC6H5, and R = 4-MeC6H5) were the most potent ones. Their HDAC inhibitory activity (IC50 values, 0.041-0.044μM) and cytotoxicity (IC50 values, 0.671-1.211μM) was approx. 2- to 3-fold more potent than suberoylanilide hydroxamic acid (SAHA). Some compounds showed up to 10-fold more potent HDAC6 inhibition compared to their inhibitory activity in total HDAC extract assay. Anal. of selected compounds II (R = 4-ClC6H5, and R = 4-MeC6H5) revealed that these compounds strongly induced both early and late apoptosis and arrested SW620 cells at the G2/M phase. Docking studies were carried out on the HDAC6 isoform for series II and revealed some important features contributing to the inhibitory activity of synthesized compounds
ACS Omega published new progress about Antitumor agents. 20776-50-5 belongs to class bromides-buliding-blocks, and the molecular formula is C7H6BrNO2, Category: bromides-buliding-blocks.
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary