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Synthesis and antitumor activities of 2‐(substituted)phenyl‐1,2,4‐triazolo[1,5‐ a ]pyridines
Author(s) -
Zhang Guolin,
Hu Yongzhou
Publication year - 2007
Publication title -
journal of heterocyclic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.321
H-Index - 59
eISSN - 1943-5193
pISSN - 0022-152X
DOI - 10.1002/jhet.5570440428
Subject(s) - chemistry , potassium hydroxide , in vitro , mtt assay , cisplatin , proton nmr , stereochemistry , potassium , carbon 13 nmr , medicinal chemistry , combinatorial chemistry , organic chemistry , biochemistry , chemotherapy , medicine , surgery
Twenty‐three 2‐(substituted)phenyl‐1,2,4‐triazolo[1,5‐ a ]pyridines have been synthesized by cycloadditison reaction between N ‐amino methylpyridinium mesitylenesulfonates and substituted benzonitriles under the presence of potassium hydroxide at room temperature. The structures of all products were confirmed by 1 H NMR, MS and elemental analyses. The antitumor activities of these compounds were evaluated against human ovary cancer cell line (HO‐8910) in vitro by MTT method. The preliminary results showed that compound 1e (IC 50 28μM) and compound 1w (IC 50 31μM) exhibited stronger antitumor activities than cisplatin (IC 50 35μM) in vitro . Hence, 1e and 1w have potential antitumor activities and are worth further investigation.