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.
Design and Synthesis of Some New 1,4-Benzoxazine-Isoxazole Hybrids as In Vitro Anticancer Agents
Benarjee,Saritha,Sailaja
, p. 1783 - 1788 (2021/11/04)
Abstract: Synthesis of twelve novel regioselective 1,4-benzoxazine-isoxazole hybrids as in vitro anticancer agents via Cu(I) catalyzed one-pot reaction of various terminal alkynes with 3-(3-oxo-2H-benzo[b][1,4]oxazin-4(3H)-yl)propanal in benign aqueous t-butanol at room temperature is presented herein. Five products have demonstrated promising activity, among those the compound 6f demonstrates outstanding activity towards PC3, A549, MCF-7, and HeLa with IC50 values of 2.61, 3.34, 2.74, and 7.04 μM respectively.
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.