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One‐Pot Synthesis of New Thiadiazolyl‐Pyridines as Anticancer and Antioxidant Agents
Author(s) -
Gomha Sobhi M.,
Muhammad Zeinab A.,
Abdelaziz Mohamad R.,
Abdelaziz Hassan M.,
Gaber Hatem M.,
Elaasser Mahmoud M.
Publication year - 2018
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.3088
Subject(s) - chemistry , antioxidant , pyridine , acetic acid , ammonium acetate , cisplatin , aldehyde , ammonium hydroxide , a549 cell , stereochemistry , organic chemistry , biochemistry , cell , catalysis , high performance liquid chromatography , medicine , surgery , chemotherapy
The reaction of one equivalents of 5‐acetylthiadiazole with one equivalent of aldehyde in acetic acid and ammonium acetate yielded thiadiazolyl‐pyridine derivatives in a multicomponent reactions. The structures of all the new compounds were elucidated on the basis of elemental analysis and spectral data. The anticancer activities of the synthesized compounds were screened for their activity against human lung carcinoma (A549) and human hepatocellular carcinoma cell lines (HepG2) comparable with cisplatin, and the results showed that most of such compounds exhibit considerable activities. The order of activity against A549 cell line was 4c , 4e , 4a , 6d , 8d , 11 , 12 , 4b , 4f , and 4d . However, compound 4e exhibited the highest activity against HepG2, followed by 4a , 4c , 6d , 8d , 11 , 12 , 4f , 4d , and 4b . On the other hand, compounds 11 , 12 , and 4b showed the highest 2,2‐diphenyl‐1‐picrylhydrazyl free radical scavenging activities. Conclusively, the results of the current study approved the cytotoxic and antioxidant capabilities of the synthesized compounds.