1237055-64-9Relevant articles and documents
Synthesis, molecular modelling studies of indolyl chalcone derivatives and their antimalarial activity evaluation
Jyoti,Gaur, Rashmi,Kumar, Yogesh,Cheema, Harveer Singh,Kapkoti, Deepak Singh,Darokar, Mahendra P.,Khan, Feroz,Bhakuni, Rajendra Singh
, p. 3261 - 3268 (2021)
Twenty one chalcone derivatives were synthesized using Claisen-Schmidt condensation, their antimalarial activity against Plasmodium falciparum was determined and quantitative structure–activity relationship (QSAR) was developed. Condensation of substituted acetophenones with various aromatic aldehydes at room temperature gave chalcones in 75–96% yield. Chalcones are secondary metabolites of terrestrial plants, precursors for the biosynthesis of flavonoids and exhibit various biological activities. Antiplasmodial IC50 (half-maximal inhibitory concentration) activity of a compound against malaria parasites in?vitro provides a good first screen for identifying the antimalarial potential of the compound. The most active compound was Trans-3-(1H-indol-3-yl)-1-(2’-hydroxyphenyl)-2-propen-1-one(1b) with IC50 of 2.1 μM/L. Molecular mechanism was explored through in silico docking & ADMET studies for the active compounds.
Chemical synthesis, docking studies and biological effects of functionalized 1,3-diaryl-2-propen-1-ones on human colon cancer cells
Zhu, Guo-Min,Huang, Guo-Dong
, p. 230 - 240 (2015)
A series of 1, 3-diaryl-2-propen-1-ones was synthesised in order to obtain a new type of anticancer drug, designed with hybrid features to inhibit colon cancer activated receptor. Based on computational modelling and docking studies, potential inhibitors were synthesised and their biological activity evaluated. The structures of newly synthesized compounds were confirmed by1HNMR,13CNMR and Mass spectrometry. All analogues were evaluated for in vitro cytotoxicity against human colon (caco-2) cancer cell lines. Compounds 1b, 1f-1h, and 2i showed significant cytotoxicity. Chalcones 1b, 1f and 1g were identified as the most potent and selective anticancer agents with IC50 values 1 μg/mL and 1.5 μg/mL, against caco-2 cell line, respectively. In conclusion, this finding confirms the suitability of indolyl chalcone analogues as candidates for further investigation towards the management of colon cancer related diseases.
Identification of Indole-Based Chalcones: Discovery of a Potent, Selective, and Reversible Class of MAO-B Inhibitors
Sasidharan, Rani,Manju, Sreedharannair Leelabaiamma,U?ar, Gülberk,Baysal, Ipek,Mathew, Bijo
, p. 627 - 637 (2016/08/27)
A series of 11 indole-based chalcones (IC1–11) with various electron donating and withdrawing groups at the para position of the phenyl ring B were synthesized. All the compounds were tested for their human monoamine oxidase (hMAO)-A and hMAO-B inhibitory