Synthesis and antitumor activity of 1, 2-benzothiazines imidazolo ［1, 2-b］［1, 3, 4］ triazazole derivatives
10.11665/j.issn.1000-5048.20190505
- VernacularTitle:含1,2-苯并噻嗪结构的咪唑并［1,2-b］［1,3,4］三氮唑衍生物的合成及其抗肿瘤活性
- Author:
Xin WANG
1
;
Xiaomei ZHAO
;
Pingping ZHANG
;
Xia JI
;
Guoqiang HU
Author Information
1. 齐鲁医药学院 药学院
- Publication Type:Journal Article
- Keywords:
imidazolo［1,2-b］［1,3,4］triazazole;
synthesize;
antitumor activity
- From:
Journal of China Pharmaceutical University
2019;50(5):540-543
- CountryChina
- Language:Chinese
-
Abstract:
In this study, triazazole moiety was introduced to piroxicam, a nonsteroidal anti-inflammatory drug, via bioisosterism to produce eight target analogs, which were structurally characterized by 1H NMR and MS. These target compounds were tested for inhibitory activities on pancreatic cancer cell(Capan-1)and leukemia cell(L1210). The results showed that compound 6b had good antiproliferative activity against Capan-1 cells(IC50=3. 6±0. 5 μmol/L); while compound 6a had good antiproliferative activity against L1210 cells(IC50=1. 8±0. 2 μmol/L), indicating that the introduction of the imidazolo［1, 2-b］［1, 3, 4］triazazole moiety could be helpful to improve the antitumor activity of these compounds.
