Synthesis, Characterization and DFT Calculations of a Novel Pyrazole Derivative 4-(1-Phenyl-5-(p-Tolyl)-2,5-Dihydro-1H-Pyrazol-3-Yl)Benzo[c][1,2,5]Oxadiazole

s Heterocyclic compounds like pyrazoline was synthesized along to the reaction of phenyl hydrazine hydrochloride with 3-(benzo [c][1,2,5] oxadiazol-4-yl)-1-phenylprop-2-en-1-one undergoing in reflux condition. This compound going to begood yields.A thoroughly fresh compound wasindicating by IR, 1H, and 13C elemental analysis. Stimulate the calculated HOMO/LUMO, MEP and mulliken population analysis and NLO was compare to the experimental analysis of this data. The optimized theoretical structure parameters betide collate to the satisfied assent with the experimental structure. Keywords: Pyrazoline, Heterocycles, NLO, HOMO/LUMO, Optimized structure, Mulliken charges. Graphical Abstract

Synthesis of a Novel Pyrano[2,3-C]pyrazole Enabling PKBβ/AKT2 Inhibitory and in Vitro Anti-Glioma Activity

<p>A series of novel pyrano[2,3-c]pyrazoles were synthesized and screened for their potential to inhibit kinases and exhibit anti-cancer activity against primary patient derived glioblastoma 2D cells and 3D neurospheres. A collection of 10 compounds were evaluated against glioma cell lines, with compound 4j exhibiting promising glioma growth inhibitory properties. Compound 4j was screened against 139 purified kinases and exhibited low micromolar activity against kinase AKT2/PKBβ. AKT signalling is one of the main oncogenic pathways in glioma and is often targeted for novel therapeutics. Indeed AKT2 levels correlated with glioma malignancy and poorer patient survival. Compound 4j inhibited the 3D neurosphere formation in primary patient derived glioma stem cells and exhibited potent EC₅₀ against glioblastoma cell lines. Herein we establish a novel biochemical kinase inhibitory function for a pyrano[2,3-c]pyrazole derivative and further report its anti-glioma activity <i>in vitro</i> for the first time.</p>

Synthesis of a Novel Pyrano[2,3-C]pyrazole Enabling PKBβ/AKT2 Inhibitory and in Vitro Anti-Glioma Activity

<p>A series of novel pyrano[2,3-c]pyrazoles were synthesized and screened for their potential to inhibit kinases and exhibit anti-cancer activity against primary patient derived glioblastoma 2D cells and 3D neurospheres. A collection of 10 compounds were evaluated against glioma cell lines, with compound 4j exhibiting promising glioma growth inhibitory properties. Compound 4j was screened against 139 purified kinases and exhibited low micromolar activity against kinase AKT2/PKBβ. AKT signalling is one of the main oncogenic pathways in glioma and is often targeted for novel therapeutics. Indeed AKT2 levels correlated with glioma malignancy and poorer patient survival. Compound 4j inhibited the 3D neurosphere formation in primary patient derived glioma stem cells and exhibited potent EC₅₀ against glioblastoma cell lines. Herein we establish a novel biochemical kinase inhibitory function for a pyrano[2,3-c]pyrazole derivative and further report its anti-glioma activity <i>in vitro</i> for the first time.</p>

Hypoglucemic Effect Exerted by an Ethynyl-Phenylamino-Steroid-Pyrazole Derivative against Glucose Levels using a Diabetic Model

The research aimed to prepare an ethynyl-phenylamino-steroid-pyrazole derivative to evaluate their hypoglycemic activity in a diabetic model using either metformin or glibenclamide as controls. Besides, a theoretical analysis was carried out to evaluate estrone derivative interaction with either insulin receptor (3iga) or potassium channel (3w12). The results showed that steroid derivatives decrease glucose levels, and this effect was in a similar form to metformin. Besides, other data suggest that the ethynyl-phenylamino-steroid-pyrazole derivative could have a higher interaction with the 3iga protein surface compared with metformin. In conclusion, the hypoglycemic activity exerted by the ethynyl-phenylamino-steroid-pyrazole derivative against glucose levels is interesting. In this way, this compound could be a good candidate for the treatment of diabetes.

Effect of Substituents of Cerium Pyrazolates and Pyrrolates on Carbon Dioxide Activation

Homoleptic ceric pyrazolates (pz) Ce(RR’pz)4 (R = R’ = tBu; R = R’ = Ph; R = tBu, R’ = Me) were synthesized by the protonolysis reaction of Ce[N(SiHMe2)2]4 with the corresponding pyrazole derivative. The resulting complexes were investigated in their reactivity toward CO2, revealing a significant influence of the bulkiness of the substituents on the pyrazolato ligands. The efficiency of the CO2 insertion was found to increase in the order of tBu2pz < Ph2pz < tBuMepz < Me2pz. For comparison, the pyrrole-based ate complexes [Ce2(pyr)6(µ-pyr)2(thf)2][Li(thf)4]2 (pyr = pyrrolato) and [Ce(cbz)4(thf)2][Li(thf)4] (cbz = carbazolato) were obtained via protonolysis of the cerous ate complex Ce[N(SiHMe2)2]4Li(thf) with pyrrole and carbazole, respectively. Treatment of the pyrrolate/carbazolate complexes with CO2 seemed promising, but any reversibility could not be observed.

STUDYING THE REACTION ROUTE OF α, β-DIBROMO KETONE AT PRESENCES OF SOME AMINES

Bromo-chalcone with containing thiene ring by the reaction of selective de­hyd­ro­bromination of α, β-dibromo ketone at presences of different amines in benzene solution and α-ethoxy-β-bromo-ketone in etha­no­lic solution in good yields were prepared. α, β-Dibromo ketone with the reaction of thiosemicarbazide le­ad to the formation of new pyrazole derivative.