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Synthesis, anti‐inflammatory, and anticancer activity evaluation of some heterocyclic amidine and bis‐amidine derivatives
Author(s) -
Sondhi Sham M.,
Rani Reshma,
Roy Partha,
Agrawal S. K.,
Saxena A. K.
Publication year - 2011
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.658
Subject(s) - amidine , chemistry , benzoxazole , hela , thiazole , benzimidazole , pyrimidine , benzothiazole , stereochemistry , combinatorial chemistry , medicinal chemistry , organic chemistry , biochemistry , in vitro
Heterocyclic amidine derivatives of benzothiazole ( 6a , 6b , 6c ), benzimidazole ( 6d , 6e , 6f ), benzoxazole ( 6g , 6h , 6i ), and bis‐amidine derivatives of pyrimidine, ( 7a , 7b ) & triazole ( 7c , 7d , 7e ) ring system have been synthesized by nucleophilic addition reaction . All these compounds were screened for anti‐inflammatory and anticancer activities. At a dose of 50 mg/kg p.o., compounds 6c (39%), 6e (39%), and 6f (39%) exhibited anti‐inflammatory activity comparable to standard drug ibuprofen, which showed 39% activity and compounds 6b , 6e , 7a , and 7c exhibited moderate anticancer activity against cervix (HELA); neuroblastoma (IMR‐32); breast (MCF‐7), leukemia (THP‐1); and cervix (HELA) human cancer cell lines, respectively. J. Heterocyclic Chem., (2011).