Synthesis, anti‐inflammatory, and anticancer activity evaluation of some heterocyclic amidine and bis‐amidine derivatives | Zendy

Sondhi Sham M. | Zendy; Rani Reshma | Zendy; Roy Partha | Zendy; Agrawal S. K. | Zendy; Saxena A. K. | Zendy

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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).

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