title: Synthesis and antitumor activity evaluation of quinazoline derivatives bearing piperazine-1-carbodithioate moiety at C4-position.
abstract: A series of quinazoline derivatives bearing piperazine-1-carbodithioate moiety at the C4-position were synthesized using piperidine and 1-bromo-3-chloropropane as starting materials via eight steps. Final compounds 8a-q and 9a-i were evaluated for their antiproliferative activity against human lung cancer A549, breast adenocarcinoma MCF-7, and colorectal cancer HCT-116 cell lines. The results showed that fourteen of twenty-six final compounds inhibited the proliferation of three cancer cell lines with IC50 values less than 10μM. When treated with a representative compound 8n, HCT-116 cells were arrested at G0/G1 phase of the cell cycle. This provided a clue to further investigation of the mechanism of action.
authors: Department of Chemistry, Capital Normal University, Beijing 100048, China.
authors: Ying
authors: Y
authors: Zhang
authors: Department of Chemistry, Capital Normal University, Beijing 100048, China.
authors: Chao-Rui
authors: CR
authors: Yang
authors: Department of Chemistry, Capital Normal University, Beijing 100048, China.
authors: Xue
authors: X
authors: Tang
authors: Department of Chemistry, Capital Normal University, Beijing 100048, China. Electronic address: slcao@cnu.edu.cn.
authors: Sheng-Li
authors: SL
authors: Cao
authors: Department of Chemistry, Capital Normal University, Beijing 100048, China.
authors: Ting-Ting
authors: TT
authors: Ren
authors: Department of Chemistry, Capital Normal University, Beijing 100048, China.
authors: Man
authors: M
authors: Gao
authors: School of Medicine, Shenzhen University, Shenzhen, Guangdong 518060, China; Beijing Key Laboratory of DNA Damage Response, College of Life Science, Capital Normal University, Beijing 100048, China.
authors: Ji
authors: J
authors: Liao
authors: School of Medicine, Shenzhen University, Shenzhen, Guangdong 518060, China; Beijing Key Laboratory of DNA Damage Response, College of Life Science, Capital Normal University, Beijing 100048, China. Electronic address: xingzhi.xu@szu.edu.cn.
authors: Xingzhi
authors: X
authors: Xu
mesh_terms: D000818:Animals; D045744:Cell Line, Tumor; D004354:Drug Screening Assays, Antitumor; D064593:Heterografts; D006801:Humans; D051379:Mice; D011799:Quinazolines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D011799:Quinazolines
keywords: Antiproliferative activity; Cell cycle; Piperazine-1-carbodithioate; Quinazoline; Synthesis