Synthesis, Cytotoxic Activity Evaluation of Novel 1, 2, 3‐Triazole Linked Quinazoline Derivatives. Issue 10 (30th June 2017)

• Record Type: Journal Article
• Authors: Song, Panpan; Cui, Fei; Li, Na; Xin, Jingchao; Ma, Qisheng; Meng, Xiangchuan; Wang, Chaojie; Cao, Qinpo; Gu, Yifei; Ke, Yu; Zhang, Qiurong; Liu, Hongmin
• Is Part Of: Chinese journal of chemistry. Volume 35:Issue 10(2017)
• Page Start: 1633
• Page End: 1639
• Publication Date: 2017-06-30
• Subjects: quinazoline -- triazole -- synthesis -- cytotoxicity; Chemistry -- Periodicals; 540.5
• DOI: 10.1002/cjoc.201700005
• Languages: English
• ISSNs: 1001-604X

Abstract

Abstract : A series of novel 1, 2, 3‐triazole‐quinazoline derivatives were synthesized in five steps starting from anthranilamide by conventional methods. All the title compounds10a —10r were evaluated for cytotoxic activity against four human cancer cell lines (MGC‐803, EC‐109, MCF‐7 and HGC‐27) using MTT assay in vitro . Some of the synthesized compounds exhibited moderate to potent activity against tested cancer cell lines. Among them, compounds10 h and10q exhibited excellent growth inhibition against HGC‐27 and compound10 m also possessed excellent activity against MCF‐7, with IC50 values less than 1 µmol/L. Especially, compound10 h was more cytotoxic than 5‐fluorouracil against all tested four human cancer cell lines. Abstract : Compounds10 h and10q exhibited excellent growth inhibition against HGC‐27 and compound10 m also possessed excellent activity against MCF‐7, with IC50 value less than 1 µmol/L. Especially, compound10 h is more cytotoxic than 5‐fluorouracil with IC50 values of 7.13, 2.17, 4.91 and 0.57 µmol/L against MCF‐7, MGC‐803, EC‐109 and HGC‐27, respectively.