5466-88-6Relevant articles and documents
Rational design, synthesis and anti-proliferative evaluation of novel 1,4-benzoxazine-[1,2,3]triazole hybrids
Bollu, Rajitha,Palem, Jyothsna Devi,Bantu, Rajashaker,Guguloth, Vijayacharan,Nagarapu, Lingaiah,Polepalli, Sowjanya,Jain, Nishant
, p. 138 - 146 (2014)
A series of novel 1,2,3-triazole-1,4-benzoxazine hybrids 5a-n were efficiently synthesized employing click chemistry approach and evaluated for anti-proliferative activity against four cancer cell lines such as HeLa (cervical), MIAPACA (pancreatic), MDA-MB-231 (breast) and IMR32 (neuroblastoma). Compounds 5n and 5g exhibited promising anti-proliferative activity with GI50 values ranging from 1.2 to 2.5 μM and 0.1-1.1 μM respectively against all cell lines, like HeLa, MDA-MB-231, MIAPACA and IMR32, while compound 5l showed significant activity against MDA-MB-231 and IMR32 with GI50 values ranging from 1.1 and 1.4 μM. This is the first report on the synthesis and in vitro anti-proliferative evaluation of 1,2,3-triazole-1,4-benzoxazine hybrids.
Quantitative helix handedness bias through a single Hvs.CH3stereochemical differentiation
Bindl, Daniel,Heinemann, Elisabeth,Mandal, Pradeep K.,Huc, Ivan
supporting information, p. 5662 - 5665 (2021/06/16)
A novel chiral aromatic δ-amino acid building block was shown to fully induce handedness in quinoline oligoamide foldamers with the possibility of further increasing the bias by combining multiples of these units in the same sequence. Through its incorporation within the helix, both N- and C-termini are still accessible for further functionalisation.
Synthesis, antimicrobial, antioxidant and docking study of novel 2H-1,4-Benzoxazin-3(4H)-One derivatives
Abdalhassan, Helen,Jabbar, Souad,Khalf, Abdul Jabar,Ibrahim, Redha,Mutanabbi, Ahmed
, p. 225 - 238 (2020/04/08)
A NOVEL series of 1,4-benzoxazinone derivatives were synthesized and characterized using FT-IR , 1H-NMR, 13C-NMR and Mass spectroscopy. These compounds were in vitro screened against several bacterial species gram positive and gram negative as well as Candida albicans and found exhibiting moderate to potent activity. The antioxidant study was confirmed for the synthesized derivatives against 1,1-diphenyl-2-picryl hydrazyl (DPPH) radical. Docking study for the potent compound 8 against glucosamine-6-phosphate synthase , the target enzyme for the antimicrobial agents was explored to explain the interactions of the discovered hits with in the amino acid residues of the enzyme active side. The docking parameters enhanced the activity of new compound as promising antimicrobial agents.