32140-74-2Relevant academic research and scientific papers
Bis-chalcone analogues as potent NO production inhibitors and as cytotoxic agents
Vijaya Bhaskar Reddy,Shen, Yuh-Chiang,Ohkoshi, Emika,Bastow, Kenneth F.,Qian, Keduo,Lee, Kuo-Hsiung,Wu, Tian-Shung
experimental part, p. 97 - 103 (2012/03/08)
Chalcones have a distinctive 1,3-diarylpropenone skeleton and exert numerous biological effects. Using a one-step Claisen-Schmidt condensation, we synthesized eleven bis-chalcones (3-13) and three acetyl chalcones (14-16) from substituted aldehydes and diacetylresorcinol. The compounds were tested for in vitro cytotoxic activity against four human cancer cell lines (A549, DU145, KB, and KB-VIN) and inhibition of NO production in lipopolysaccharide (LPS)-activated microglial cells. Among them, four compounds (3, 5, 6, and 13) showed significant cytotoxic activity with EC50 values ranging from 1.57 to 5.14 μM, and seven compounds (3, 5-8, 10, and 13) displayed potent anti-inflammatory activity by inhibiting NO production with IC50 values ranging from 0.95 to 8.65 μM. A mechanism of action study of active compounds 6 and 7 discovered that these compounds down-regulated iNOS expression by inhibiting p65 NF-κB activation/nuclear translocation due to prevention of IκBα degradation. Structure-activity relationship (SAR) findings are also discussed.
Synthesis of 4,6-Bis(2'-substituted-2',3'-dihydro-1,5-benzothiazepin-4'-yl) resorcinols as potential antifeedants
Reddy, R Jayasimha,Ashok, D,Sarma, P N
, p. 404 - 406 (2007/10/02)
4,6-Bis(2'-substituted-2',3'-dihydro-1,5-benzothiazepin-4'-yl) resorcinols (3a-j) have been prepared in one step by the reaction of dichalcones (2a-j) with 2-aminothiophenol in ethanol containing gl. acetic acid and their structures established by element
