Details

Autor(en) / Beteiligte

• Gondru, Ramesh
• Saini, Ratni
• Vaarla, Krishnaiah
• Singh, Sarika
• Sirassu, Narsimha
• Bavantula, Rajitha
• Saxena, Anil K.

Titel

Synthesis and Characterization of Chalcone‐Pyridinium Hybrids as Potential Anti‐Cancer and Anti‐Microbial Agents

Ist Teil von

• ChemistrySelect (Weinheim), 2018-02, Vol.3 (5), p.1424-1431

Erscheinungsjahr

2018

Quelle

Wiley Online Library

Beschreibungen/Notizen

• A series of pyridinium salts (5 a‐p) have been synthesized and were screened for their in vitro anticancer activity against MCF‐7 (breast cancer), HeLa (cervical cancer), U‐87MG (human glioblastoma) and HEK293 (Human Embryonic Kidney 293 cells) cell lines by taking doxorubicin as a positive control. The compounds derived from 4‐methoxyphenyl (5 c) and 4‐nitrophenyl (5 h) have showed significant and broad spectrum antiproliferative activity against the tested cancer cell‐lines and also displayed potential in vivo against Ehrlich ascites carcinoma (EAC) in mice. Also, screened the compounds for their antimicrobial and anti‐acetylcholinesterase (anti‐AchE) activities. It was observed form the in vitro results that, compounds derived from 4‐methylphenyl (5 b), 4‐chlorophenyl (5 f), coumarinyl (5 i) and napthyl (5 j) have exhibited potential antibacterial activity against Staphylococcus aureus and the derivatives 5 b and 4‐fluorophenyl (5 e) have showed promising antifungal activity and the compound 5 c showed moderate AChE inhibitory activity. A series of chalcone‐pyridinium bromide hybrids (5 a‐p) were synthesized. Assessed for in vitro biological activities: anticancer (in vivo and in vivo) and antimicrobial activity and AchE‐inhibiting activity. In vitro and in vivo antitumor studies confirmed that, the compounds 5 c and 5 h were possessing potential antitumor activity. The compounds 5 b, 5 f, 5 i and 5 j may serve as a potential lead compounds for the development of anti‐bacterial agents, particularly against Staphylococcus aureus.