Synthesis and antitumor activities of 1, 2-benzothiazines［1, 3, 4］thiadiazolo［3, 2-a］［1, 3, 5］triazin derivatives

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

doi:10.11665/j.issn.1000-5048.20200104

Journal of China Pharmaceutical University > 2020 > 51(1): 24-28. > DOI: 10.11665/j.issn.1000-5048.20200104

ZHAO Xiaomei, WANG Xin, JI Xia, ZHANG Hua, ZHANG Pingping, HU Guoqiang. Synthesis and antitumor activities of 1, 2-benzothiazines［1, 3, 4］thiadiazolo［3, 2-a］［1, 3, 5］triazin derivatives[J]. Journal of China Pharmaceutical University, 2020, 51(1): 24-28. DOI: 10.11665/j.issn.1000-5048.20200104

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Synthesis and antitumor activities of 1, 2-benzothiazines［1, 3, 4］thiadiazolo［3, 2-a］［1, 3, 5］triazin derivatives

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Based on the drug design principle of reactive functional group splicing, nine novel title compounds were designed and synthesized with piroxicam intermediate as the starting material. Their structures were characterized by ¹H NMR and MS analysis. The in vitro antitumor activity evaluation suggested that compounds 6f , 6h and 6g exhibited good inhibitory reactivity on pancreatic cancer cell line Capan-1(IC₅₀=2. 4±0. 5 μmol/L), leukemia cell line L1210(IC₅₀=5. 4±0. 2 μmol/L), and human liver cancer cell line SMMC-7721(IC₅₀=3. 8±0. 2 μmol/L), respectively. The introduction of thiadiazolo［3, 2-a］triazine side chain could improve the antitumor activity of these compounds.
- ［1,3,4］ thiadiazolo［3,2-a］［1,3,5］triazin,
- synthesis,
- antitumor activity

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Synthesis and antitumor activities of 1, 2-benzothiazines［1, 3, 4］thiadiazolo［3, 2-a］［1, 3, 5］triazin derivatives

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