Rational design, synthesis and anti-proliferative evaluation of novel 1,4-benzoxazine-[1,2,3]triazole hybrids

Synthesis, Characterization, and Antibacterial Activity of Diethyl 1-((4-Methyl-2-phenyl-4,5-dihydrooxazol-4-yl)methyl)-1H-1,2,3-triazole-4,5-dicarboxylate

“…1,2,3-Triazoles are an important class of heterocyclic compounds due to their wide usage as synthetic intermediates and pharmaceuticals [1][2][3]. Many triazole derivatives are found to exhibit various pharmacological properties such as antimicrobial [4], antiepileptic [5], antitubercular [6], and antibacterial [7], and a large number of 1,2,3-triazoles have also been reported with significant anticancer activities [8][9][10]. Since they are nontoxic, highly stable compounds and mostly water soluble, the 1,2,3-triazole derivatives could be ideal drug candidate and they could participate actively in molecular interactions by hydrogen bond formation [11] which implies their facility to binding with the biological targets [12].…”

Design, Synthesis, and Evaluation of the Kinase Inhibition Potential of Pyridylpyrimidinylaminophenyl Derivatives

“…1) [26] conserved in its structure; the drug is efficacious in imatinib resistant cases [27]. On the basis of above and considering the literature reports discussing Abl-imatinib structural interactions [16,[26][27][28][29][30][31][32], we decided to conjugate the scaffolds based on 2-pyridone [21,33,34], benzopyran-2-one [35], benzopyran-4-one [22,36], indole acetic acid, iso-nicotinic acid, hippuric acid, piperic acid, 2-oxoquinolinacetic acid, 3-oxobenzooxazinacetic acid [37], and trimethoxyphenyl acrylic acid [38], with PPAP moiety to form the amide/cyclic amide derivatives.…”

Synthesis of isoindolo[1,4]benzoxazinone and isoindolo[1,5]benzoxazepine: two new ring systems of pharmaceutical interest

“…5 Also benzoxazepine derivatives are well-known pharmacophores showing promising properties against various diseases such as antipsychotic, 6 central nervous system, 7 and anti-cancer activities. 8 Variously substituted pyrrolo [1,5]benzoxazepines have shown antiproliferative activity in a wide range of tumor cell lines at micromolar concentrations. They have been identified as novel microtubule-targeting agents that possess the ability to potently to induce cell cycle arrest and apoptosis against solid tumors and hematological malignancies.…”

“…31 In this paper, continuing our studies on isoindole systems, 32,33 we report the synthesis of derivatives of two new ring systems isoindolo[1,4]benzoxazinone 5 and isoindolo [1,5]benzoxazepine 8e10 and the antiproliferative activity of some of them against a wide range of human tumor cell lines at low micromolar level.…”

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a b s t r a c tTwo new ring systems, isoindolo[1,4]benzoxazinone and isoindolo [1,5]benzoxazepine, were conveniently synthesized through cyclization of suitably substituted isoindole derivatives. Some of the new compounds exhibited antiproliferative activity against a wide range of human tumor cell lines with GI 50 mean values at low micromolar level (3.72e5.13 mM).

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