Synthesis and antitumor activity of 1, 2-benzothiazines imidazolo ［1, 2-b］［1, 3, 4］ triazazole derivatives

WANG Xin; ZHAO Xiaomei; ZHANG Pingping; JI Xia; HU Guoqiang

doi:10.11665/j.issn.1000-5048.20190505

Journal of China Pharmaceutical University > 2019 > 50(5): 540-543. > DOI: 10.11665/j.issn.1000-5048.20190505

WANG Xin, ZHAO Xiaomei, ZHANG Pingping, JI Xia, HU Guoqiang. Synthesis and antitumor activity of 1, 2-benzothiazines imidazolo ［1, 2-b］［1, 3, 4］ triazazole derivatives[J]. Journal of China Pharmaceutical University, 2019, 50(5): 540-543. DOI: 10.11665/j.issn.1000-5048.20190505

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Synthesis and antitumor activity of 1, 2-benzothiazines imidazolo ［1, 2-b］［1, 3, 4］ triazazole derivatives

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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.
- imidazolo［1,2-b］［1,3,4］triazazole,
- synthesize,
- antitumor activity

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Synthesis and antitumor activity of 1, 2-benzothiazines imidazolo ［1, 2-b］［1, 3, 4］ triazazole derivatives

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