35458-14-1Relevant academic research and scientific papers
Modular synthesis and antiproliferative activity of new dihydro-1H-pyrazolo[1,3-b]pyridine embelin derivatives
Amesty, ángel,Estévez-Braun, Ana,Fernández-Pérez, Leandro,Guerra, Borja,Guerra-Rodríguez, Miguel,Martín-Acosta, Pedro
, (2021/10/22)
A set of new dihydro-1H-pyrazolo[1,3-b]pyridine and pyrazolo[1,3-b]pyridine embelin derivatives was synthesized through a multicomponent reaction from natural embelin, 3-substituted-5-aminopyrazoles and aldehydes. The synthesized compounds were evaluated against three hematologic tumor cell lines, HEL (acute erythroid leukemia), K-562 (chronic myeloid leukemia) and HL-60 (acute myeloid leukemia), and five breast cancer cell lines (SKBR3, MCF-7, MDA-MB-231, BT-549, HS-578T). The primate non-malignant kidney Vero cell line was used as the control of cytotoxicity. From the obtained results, some structure–activity relationships were out-lined. Furthermore, in silico prediction of physicochemical properties and ADME parameters were determined for the derivatives with the best antiproliferative values.
A new family of densely functionalized fused-benzoquinones as potent human protein kinase CK2 inhibitors
Martín-Acosta, Pedro,Haider, Samer,Amesty, ángel,Aichele, Dagmar,Jose, Joachim,Estévez-Braun, Ana
, p. 410 - 423 (2018/01/01)
A new series of 2-amino-4-phenyl-6-hydroxy-7-alkyl-pyranobenzoquinones was synthesized as ATP-competitive CK2 inhibitors. They were readily synthesized through a three-component Knoevenagel condensation-Michael addition-heterocyclization reaction from ald
Novel series of benzoquinones with high potency against 5-lipoxygenase in human polymorphonuclear leukocytes
Filosa, Rosanna,Peduto, Antonella,Schaible, Anja M.,Krauth, Verena,Weinigel, Christina,Barz, Dagmar,Petronzi, Carmen,Bruno, Ferdinando,Roviezzo, Fiorentina,Spaziano, Giuseppe,D'Agostino, Bruno,De Rosa, Mario,Werz, Oliver
supporting information, p. 132 - 139 (2015/04/14)
5-Lipoxygenase (5-LO) is a potential target for pharmacological intervention with various inflammatory and allergic diseases. Starting from the natural dual 5-LO/microsomal prostaglandin E2 synthase (mPGES)-1 inhibitor embelin (2,5-dihydroxy-3-
Discovery of a novel inhibitor of NAD(P)+-dependent malic enzyme (ME2) by high-throughput screening
Wen, Yi,Xu, Lei,Chen, Fang-Lei,Gao, Jing,Li, Jing-Ya,Hu, Li-Hong,Li, Jia
, p. 674 - 684 (2015/06/30)
Aim: Malic enzymes are oxidative decarboxylases with NAD+ or NAD(P)+ as cofactor that catalyze the conversion of L-malate to pyruvate and CO2. The aim of this study was to discover and characterize a potent inhibitor of hu
