Details

Autor(en) / Beteiligte

• Lan, Ta Thu
• Anh, Duong Tien
• Pham-The, Hai
• Dung, Do Thi Mai
• Park, Eun Jae
• Jang, Sun Dong
• Kwon, Joo Hee
• Kang, Jong Soon
• Thuan, Nguyen Thi
• Han, Sang-Bae
• Nam, Nguyen-Hai

Titel

Design, Synthesis and Bioevaluation of Two Series of 3-((1-Benzyl-1H-1,2,3-triazol-4-yl)methyl)quinazolin-4(3H)-ones and N-(1-benzylpiperidin-4-yl)quinazolin-4-amines

Ist Teil von

• Chemistry & biodiversity, 2020-05

Ort / Verlag

Switzerland

Erscheinungsjahr

2020

Quelle

Wiley Online Library

Beschreibungen/Notizen

• Two series of 3-((1-benzyl-1 H -1,2,3-triazol-4-yl)methyl)quinazolin-4(3H)-ones ( 4a-j ) and N-(1-benzylpiperidin-4-yl)quinazolin-4-amines ( 6a-j ) were designed initially as potential acetylcholine esterase inhibitors. Biological evaluation demonstrated that series 6a-j significantly inhibited AChE activity. Especially compounds 6c and 6e were found to be the most potent with relative AChE inhibition percentages of 87% in comparison to donepezil. The docking studies with AChE showed similar interactions between Donepezil and these four derivatives. Compounds 6a-j also exhibited significant DPPH scavenging effects. Two compound series also exerted moderate to good cytotoxicity againsts three human cancer cell lines, including SW620 (human colon cancer), PC-3 (prostate cancer), and NCI-H23 (lung cancer), with compound 4a being the most cytotoxic agent. Compound 4a significantly induced early apoptosis and arrested the SW620 cells at G2/M phase. From this study, compounds 6c and 6e could serve as new leads for further design and AChE inhibitors, while compound 4a could serve as a new lead for the design and development of more potent anticancer agents.