213920-30-0Relevant academic research and scientific papers
Design, synthesis and biological evaluation of some novel 3-cinnamoyl-4-hydroxy-2H-chromen-2-ones as antimalarial agents
Patel, Kuldeep,Karthikeyan, Chandrabose,Hari Narayana Moorthy, N. S.,Deora, Girdhar Singh,Trivedi, Piyush,Solomon, Viswas Raja,Lee, Hoyun
, p. 1780 - 1784,5 (2020/07/30)
A novel series of 3-cinnamoyl-4-hydroxy-2Hchromen-2-ones were designed, synthesized and screened for antiplasmodial activity. Eleven compounds of the series exhibited micromolar potency against chloroquine sensitive and chloroquine resistant strains. The most potent compound 4-hydroxy-3-(3-(4- nitrophenyl)acryloyl)-2Hchromen-2-one showed inhibitory potency (IC 50) of 3.1 and 4 μg/ml against chloroquine sensitive and chloroquine resistant strains, respectively. A structure activity relationship study was performed by correlating the effect of substituents with the antimalarial activity of the title compounds. The novel 3-cinnamoyl-4-hydroxy- 2H-chromen-2-ones reported here should be good lead for further development of antimalarial agents that can overcome resistance.
Evaluation of Structurally Diverse Benzoazepines Clubbed with Coumarins as Mycobacterium tuberculosis Agents
Upadhyay, Kuldip,Manvar, Atul,Shah, Anamik,Rawal, Kena,Joshi, Sudhir,Trivedi, Jalpa,Chaniyara, Ravi
, p. 1003 - 1008,6 (2012/12/12)
Tuberculosis caused by Mycobacterium tuberculosis remains a leading cause of mortality worldwide into 21st century. In continuation with our anti-tuberculosis research programme, in this work, we have prepared molecularly diverse coumarins clubbed with benzothiazepines as well as its aza-analogues-benzodiazepines by molecular hybridization. The resulting compounds were screened for their M. tuberculosis activity against H37Rv strains using microplate alamar blue assay. Among the designed diversity, the compounds 5k, 5n and 5o were found significantly active in primary anti-tuberculosis assay at minimum inhibitory concentration 50 values of 5k and 5o in level-2 screening were observed as >10μg/mL and 3.63μg/mL, respectively. Design and synthesis of more focused library and its three-dimensional quantitative structure activity relationship analysis are underway. In the present work, various coumarins clubbed with benzo(thi)diazepines were evaluated for their M. tuberculosis activity against H37Rv strains using MABA assay. The IC50 values of two analogs (compounds 5k and 5o) in level-2 screening were observed as >10μg/mL and 3.63μg/mL respectively.
Synthesis of some coumarinyl chalcones and their antiproliferative activity against breast cancer cell lines
Patel, Kuldeep,Karthikeyan, Chandrabose,Solomon, Viswas Raja,Moorthy, N.S. Hari Narayana,Lee, Hoyun,Sahu, Kapendra,Deora, Girdhar Singh,Trivedi, Piyush
, p. 308 - 311 (2012/05/05)
A series of coumarinyl chalcones derivatives were synthesized and evaluated for their antiproliferative activities on three different breast cancer cell lines (MDA-MB231, MDA-MB468, MCF7) and one non-cancer breast epithelial cell line (184B5). The coumarinyl derivatives exhibited anticancer activity against breast cancer cell lines at a micromolar range. A structure-activity relationship (SAR) analysis was performed by studying the effect of substituents on their antiproliferative activities. One of the compound 3i bearing methoxy substitutions at the R1; R2 and R3 positions of the phenyl ring showed comparable potency to the reference drug cisplatin as well as a two-fold higher selectivity for the breast cancer cell lines than 184B5 cells.
