Category: 574-98-1

Fonseca-Berzal, Cristina; Ibanez-Escribano, Alexandra; Vela, Nerea; Cumella, Jose; Nogal-Ruiz, Juan Jose; Escario, Jose Antonio; Bernardino da Silva, Patricia; Batista, Marcos Meuser; Soeiro, Maria de Nazare C.; Sifontes-Rodriguez, Sergio; Meneses-Marcel, Alfredo; Gomez-Barrio, Alicia; Aran, Vicente J. published an article in 2018, the title of the article was Antichagasic, Leishmanicidal, and Trichomonacidal Activity of 2-Benzyl-5-nitroindazole-Derived Amines.Recommanded Product: 574-98-1 And the article contains the following content:

Three different series of new 5-nitroindazole derivatives-1-(ω-aminoalkyl)-2-benzylindazolin-3-ones (series A; ten compounds), 3-(ω-aminoalkoxy)-2-benzylindazoles (series B; four compounds) and 3-alkylamino-2-benzylindazoles (series C; five compounds)-have been synthesized and evaluated against the protozoan parasites Trypanosoma cruzi, Leishmania amazonensis, and Trichomonas vaginalis: etiol. agents of Chagas disease, cutaneous leishmaniasis, and trichomoniasis, resp. Many indazoles of series A, B, and C were efficient against T. cruzi. Some compounds in series A, after successfully passing the preliminary screening for epimastigotes, exhibited activity values against amastigotes of several T. cruzi strains that were better than or similar to those shown by the reference drug benznidazole and displayed low nonspecific toxicity against mammalian cells. On the other hand, preliminary studies against promastigotes of L. amazonensis showed high leishmanicidal activity for some derivatives of series A and C. With regard to activity against T. vaginalis, some indazoles of series B and C were rather efficient against trophozoites of a metronidazole-sensitive isolate and showed low nonspecific toxicities toward Vero cell cultures. Addnl., some of these compounds displayed similar activity against metronidazole-sensitive and resistant isolates, showing the absence of cross-resistance between these derivatives and the reference drug. The experimental process involved the reaction of 2-(2-Bromoethyl)isoindoline-1,3-dione(cas: 574-98-1).Recommanded Product: 574-98-1

The Article related to benzyl nitroindazole amine antichagasic leishmanicidal trichomonacidal activity, antiprotozoal agents, leishmaniasis, nitrogen heterocycles, trichomoniasis, trypanosomiasis and other aspects.Recommanded Product: 574-98-1

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Halik, Pawel K.; Lipinski, Piotr F. J.; Matalinska, Joanna; Kozminski, Przemyslaw; Misicka, Aleksandra; Gniazdowska, Ewa published an article in 2020, the title of the article was Radiochemical synthesis and evaluation of novel radioconjugates of neurokinin 1 receptor antagonist aprepitant dedicated for NK1R-positive tumors.Recommanded Product: 574-98-1 And the article contains the following content:

Aprepitant, a lipophilic and small mol. representative of neurokinin 1 receptor antagonists, is known for its anti-proliferative activity on numerous cancer cell lines that are sensitive to Substance P mitogen action. In the presented research, we developed two novel structural modifications of aprepitant to create aprepitant conjugates with different radionuclide chelators. All of them were radiolabeled with 68Ga and 177Lu radionuclides and evaluated in terms of their lipophilicity and stability in human serum. Furthermore, fully stable conjugates were examined in mol. modeling with a human neurokinin 1 receptor structure and in a competitive radioligand binding assay using rat brain homogenates in comparison to the aprepitant mol. This initial research is in the conceptual stage to give potential theranostic-like radiopharmaceutical pairs for the imaging and therapy of neurokinin 1 receptor-overexpressing cancers. The experimental process involved the reaction of 2-(2-Bromoethyl)isoindoline-1,3-dione(cas: 574-98-1).Recommanded Product: 574-98-1

The Article related to aprepitant radiopharmaceutical neurokinin receptor antagonist radionuclide chelator, aprepitant, neurokinin 1 receptor antagonist, radionuclide chelators, radiopharmaceuticals and other aspects.Recommanded Product: 574-98-1

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On April 1, 2021, Ibanez-Escribano, Alexandra; Reviriego, Felipe; Vela, Nerea; Fonseca-Berzal, Cristina; Nogal-Ruiz, Juan Jose; Aran, Vicente J.; Escario, Jose Antonio; Gomez-Barrio, Alicia published an article.Quality Control of 2-(2-Bromoethyl)isoindoline-1,3-dione The title of the article was Promising hit compounds against resistant trichomoniasis: Synthesis and antiparasitic activity of 3-(ω-aminoalkoxy)-1-benzyl-5-nitroindazoles. And the article contained the following:

A series of 11 3-(ω-aminoalkoxy)-1-benzyl-5-nitroindazoles has been prepared starting from 1-benzyl-5-nitroindazol-3-ol, and evaluated against sensitive and resistant isolates of the sexually transmitted protozoan Trichomonas vaginalis. A variety of nitroindazoles demonstrate trichomonacidal profiles with IC50 < 20μM against the metronidazole-sensitive isolate. Moreover, all these compounds submitted to cytotoxicity assays against mammalian cells exhibited low non-specific cytotoxic effects, except two compounds I and II which displayed moderate cytotoxicity (CC50 = 74.7 and 59.1μM, resp.). Those compounds with trichomonacidal effect were also evaluated against a metronidazole-resistant culture. Special mention deserve compounds III and IV, which displayed better IC50 values (1.3 and 0.5μM resp.) than that of the reference drug (IC50 MTZ = 3.0μM). The high activity of these compounds against the resistant isolate reinforces the absence of cross-resistance with the reference drug. The remarkable trichomonacidal results against resistant T. vaginalis isolates suggest the interest of 3-(ω-aminoalkoxy)-1-benzyl-5-nitroindazoles to be considered as good prototypes to continue in the development of new drugs with enhanced trichomonacidal activity, aiming to increase the non-existent drugs to face clin. resistance efficiently for those patients in whom therapy with 5-nitroimidazoles is contraindicated. The experimental process involved the reaction of 2-(2-Bromoethyl)isoindoline-1,3-dione(cas: 574-98-1).Quality Control of 2-(2-Bromoethyl)isoindoline-1,3-dione

The Article related to aminoalkoxy benzyl nitroindazole preparation antiparasitic resistant trichomoniasis, antiprotozoal agents, indazole, nitrogen heterocycles, resistance, trichomonas vaginalis and other aspects.Quality Control of 2-(2-Bromoethyl)isoindoline-1,3-dione

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On July 31, 2022, Xu, Ying; Chen, Peng; Tang, Lei; Zhang, Xiaojun; Shi, Feng; Ning, Xuyang; Bi, Jingli; Qu, Yang; Liu, Hongfei published an article.Electric Literature of 574-98-1 The title of the article was Hypoxia responsive and tumor-targeted mixed micelles for enhanced cancer therapy and real-time imaging. And the article contained the following:

Most chemotherapy agents have serious side effects due to lack of tumor targeting, which affects their clin. application. In addition, as an essential characteristic of malignant tumor, hypoxia is attracting exclusive research focus regarding its non-invasive real-time tracing in novel targeting delivery system. Herein, we designed a mixed micelle with tumor targeting and hypoxia responsiveness for tumor therapy and imaging. In particular, the dual-modified mix micelles were self-assembled by folic acid (FA) and 2-(2-nitroimidazole) ethylamine (NI) conjugated polymers, in which paclitaxel (PTX) and quantum dots (QDs) were co-loaded into the hydrophobic core. The drug loaded micelles showed satisfactory drug encapsulation, good storage stability, and sustained release properties. In vitro cell experiments showed that the mixed micelles exhibited enhanced cytotoxic effect and improved the cellular uptake, especially under hypoxic conditions, which was due to the FA mediated active targeting effect and NI induced hypoxic responsive release. In vivo experiments further proved that the mixed micelles possessed outstanding tumor targeting and hypoxia responsive properties. Furthermore, the drug loaded micelles showed excellent anti-tumor effect and can realize real-time in vivo imaging. This work demonstrates that the dual-modified mixed micelles co-loading with PTX and QDs might provide a novel approach for tumor therapy and imaging. The experimental process involved the reaction of 2-(2-Bromoethyl)isoindoline-1,3-dione(cas: 574-98-1).Electric Literature of 574-98-1

The Article related to folic acid nitroimidazoleethylamine polymer hypoxia tumor targeted micelle antitumor, hypoxia responsiveness, paclitaxel, quantum dots, real-time imaging, targeted deliver and other aspects.Electric Literature of 574-98-1

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On March 31, 2020, Rodriguez-Cruz, Mario A.; Hernandez-Ortega, Simon; Valdes, Hugo; Rufino-Felipe, Ernesto; Morales-Morales, David published an article.Category: bromides-buliding-blocks The title of the article was C-S cross-coupling catalyzed by a series of easily accessible, well defined Ni(II) complexes of the type [(NHC)Ni(Cp)(Br)]. And the article contained the following:

The synthesis, characterization and catalytic evaluation of a series of NHC-Ni(II) complexes I [R = Me, n-Bu, Bn] bearing a phthalimide fragment and a cyclopentadienyl (Cp) ligand was reported. The complexes were evaluated in C-S couplings of iodobenzene and a range of thiols to give thioethers R1-S-R2 [R1 = Ph; R2 = t-Bu, 4-FC6H4, 2-naphthyl, etc.]. The reactions were carried out using a catalyst loading of 5 mol % in DMF during 0.5-19 h. Complex I [R = n-Bu] was the one exhibited the best activity for these transformations yielding up to 96% of products in 0.5 h. The experimental process involved the reaction of 2-(2-Bromoethyl)isoindoline-1,3-dione(cas: 574-98-1).Category: bromides-buliding-blocks

The Article related to nhc based nickel complex preparation, thioether preparation, thiol iodobenzene carbon sulfur cross coupling nickel catalyst, Benzene, Its Derivatives, and Condensed Benzenoid Compounds: Phenols, Thiophenols, and Derivatives Including Phenol and Thiophenol Ethers and Esters and other aspects.Category: bromides-buliding-blocks

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On February 28, 2022, Li, Zhi-Ying; Xu, Guang-Sen; Song, Yu-Liang; Li, Xun published an article.Application of 574-98-1 The title of the article was Structural optimizations and bioevaluation of N-substituted acridone derivatives as strong topoisomerase II inhibitors. And the article contained the following:

Previously, an array of N-substituted acridone derivatives have been reported as potent topoisomerase II (topo II) inhibitors, and preliminary structure-activity relationship (SAR) outcomes revealed that the linker between 1-NH and N-Me piperazine motif of the tricyclic acridone scaffold significantly affected their anti-proliferative potencies. To further explore the SARs of acridone-derived topo II inhibitors, a wider range of novel acridone derivatives were herein synthesized via two rounds of structural optimizations on two validated hits, E17 and E24. Initially, the linker length was optimized, and then influences of N-Me piperazinyl moiety and disposition of three N atoms on the bioactivity were investigated. As a result, a newly developed topo II inhibitor 6 h was found to be more potent than E17 and E24, thereby serving as a tool compound for the follow-up mechanistic study. Compound 6 h functioned as a strong topo IIα/β inhibitor, caused obvious DNA damage, and induced apoptosis by triggering the loss of mitochondrial membrane potential (Δψm). Further mol. docking and MD study illustrated the favorable interactions of 6 h with both topo IIα and topo IIβ subtypes. The experimental process involved the reaction of 2-(2-Bromoethyl)isoindoline-1,3-dione(cas: 574-98-1).Application of 574-98-1

The Article related to topoisomerase ii inhibitors structure activity relationship anticancer, n-substituted acridone derivatives, structural optimization, structure-activity relationship, topo iiα/β inhibitor and other aspects.Application of 574-98-1

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Czopek, Anna; Partyka, Anna; Bucki, Adam; Pawlowski, Maciej; Kolaczkowski, Marcin; Siwek, Agata; Gluch-Lutwin, Monika; Koczurkiewicz, Paulina; Pekala, Ezzbieta; Jaromin, Anna; Tyliszczak, Bozena; Wesolowska, Anna; Zagorska, Agnieszka published an article in 2020, the title of the article was Impact of N-alkylamino substituents on serotonin receptor (5-HTR) affinity and phosphodiesterase 10A (PDE10A) inhibition of isoindole-1,3-dione derivatives.SDS of cas: 574-98-1 And the article contains the following content:

In this study, a series of compounds derived from 1H-isoindole-1,3(2H)-dione I (R = H, OMe; R1 = 1,2,3,4-tetrahydroisoquinolin-2-yl, 1,2,3,4-tetrahydroisoquinolin-2-yl, pyridin-2-yl, 1H-1,3-benzimidazol-2-yl, etc.; X = (CH2)n, n = 1-5), potential ligands of phosphodiesterase 10A and serotonin receptors, were investigated as potential antipsychotics. A library of I with various amine moieties was synthesized and examined for their phosphodiesterase 10A (PDE10A)-inhibiting properties and their 5-HT1A and 5-HT7 receptor affinities. Based on in vitro studies, the most potent compound, I [R = OMe; R1 = 1H-1,3-benzimidazol-2-yl; n = 4 (II)], was selected and its safety in vitro was evaluated. In order to explain the binding mode of compound II in the active site of the PDE10A enzyme and describe the mol. interactions responsible for its inhibition, computer-aided docking studies were performed. The potential antipsychotic properties of compound II in a behavioral model of schizophrenia were also investigated. The experimental process involved the reaction of 2-(2-Bromoethyl)isoindoline-1,3-dione(cas: 574-98-1).SDS of cas: 574-98-1

The Article related to isoindoledione preparation phosphodiesterase inhibition serotonin receptor affinity antitumor activity, antipsychotic activity, benzimidazole derivatives, phosphodiesterase 10a, schizophrenia and other aspects.SDS of cas: 574-98-1

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On May 1, 2020, Varano, Flavia; Catarzi, Daniela; Vincenzi, Fabrizio; Pasquini, Silvia; Pelletier, Julie; Lopes Rangel Fietto, Juliana; Espindola Gelsleichter, Nicolly; Sarlandie, Marine; Guilbaud, Audrey; Sevigny, Jean; Varani, Katia; Colotta, Vittoria published an article.Recommanded Product: 574-98-1 The title of the article was Structural investigation on thiazolo[5,4-d]pyrimidines to obtain dual-acting blockers of CD73 and adenosine A2A receptor as potential antitumor agents. And the article contained the following:

Adenosine pathway, including its generating enzyme (CD73) and its receptors represents a key target for cancer immunotherapy. Here we aimed to search for novel compounds able to co-target the CD73 and the A2A adenosine receptor (A2A AR) as dual-blockers of adenosine generation and activity. The design project was to combine in the same mol. the thiazolo[5,4-d]pyrimidine core, an essential pharmacophoric feature to block the A2A AR, with a benzenesulfonamide group which is a characteristic group of CD73 inhibitors. Most of the reported compounds resulted in inverse agonists of the human (h) A2A AR endowed with high affinity, selectivity and potency. However they were weak inhibitors of CD73 enzyme. Nevertheless, this study can be considered as a starting point to develop more active compounds The experimental process involved the reaction of 2-(2-Bromoethyl)isoindoline-1,3-dione(cas: 574-98-1).Recommanded Product: 574-98-1

The Article related to cancer immunotherapy a2aar inverse agonists cd37 inhibitor antitumor agents, adenosine a(2a) receptor inverse agonists, antitumor agents, cd73 inhibitors, cancer immunotherapy, thiazolo[5,4-d]pyrimidine and other aspects.Recommanded Product: 574-98-1

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On August 7, 2018, Orteca, Giulia; Tavanti, Francesco; Bednarikova, Zuzana; Gazova, Zuzana; Rigillo, Giovanna; Imbriano, Carol; Basile, Valentina; Asti, Mattia; Rigamonti, Luca; Saladini, Monica; Ferrari, Erika; Menziani, Maria Cristina published an article.Reference of 2-(2-Bromoethyl)isoindoline-1,3-dione The title of the article was Curcumin derivatives and Aβ-fibrillar aggregates: An interactions’ study for diagnostic/therapeutic purposes in neurodegenerative diseases. And the article contained the following:

Several neurodegenerative diseases, like Alzheimer’s (AD), are characterized by amyloid fibrillar deposition of misfolded proteins, and this feature can be exploited for both diagnosis and therapy design. In this paper, structural modifications of curcumin scaffold were examined in order to improve its bioavailability and stability in physiol. conditions, as well as its ability to interfere with β-amyloid fibrils and aggregates. The acid-base behavior of curcumin derivatives, their pharmacokinetic stability in physiol. conditions, and in vitro ability to interfere with Aβ fibrils at different incubation time were investigated. The mechanisms governing these phenomena have been studied at at. level by means of mol. docking and dynamic simulations. Finally, biol. activity of selected curcuminoids has been investigated in vitro to evaluate their safety and efficiency in oxidative stress protection on hippocampal HT-22 mouse cells. Two aromatic rings, π-conjugated structure and H-donor/acceptor substituents on the aromatic rings showed to be the sine qua nonstructural features to provide interaction and disaggregation activity even at very low incubation time (2 h). Computational simulations proved that upon binding the ligands modify the conformational dynamics and/or interact with the amyloidogenic region of the protofibril facilitating disaggregation. Significantly, in vitro results on hippocampal cells pointed out protection against glutamate toxicity and safety when administered at low concentrations (1 μM). On the overall, in view of its higher stability in physiol. conditions with respect to curcumin, of his rapid binding to fibrillar aggregates and strong depolymerizing activity, phthalimide derivative K2F21 appeared a good candidate for both AD diagnostic and therapeutic purposes. The experimental process involved the reaction of 2-(2-Bromoethyl)isoindoline-1,3-dione(cas: 574-98-1).Reference of 2-(2-Bromoethyl)isoindoline-1,3-dione

The Article related to curcumin neurodegenerative disease antialzheimer alzheimer diagnosis, alzheimer’s disease, amyloid β fibrillar aggregates, curcumin-derivatives, hippocampal ht-22 mouse cells, molecular dynamics simulations and other aspects.Reference of 2-(2-Bromoethyl)isoindoline-1,3-dione

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On April 30, 2019, Xie, Ruliang; Mei, Xiangdong; Ning, Jun published an article.Quality Control of 2-(2-Bromoethyl)isoindoline-1,3-dione The title of the article was Design, synthesis and insecticide activity of novel acetylcholinesterase inhibitors: triazolinone and phthalimide heterodimers. And the article contained the following:

A new series of 1,2,4-triazolin-3-one and phthalimide heterodimers I [X = (CH2)n; n = 1, 2, 9, etc.] was synthesized and evaluated for their insecticidal and acetylcholinesterase inhibitory activities. Most of the synthesized compounds I showed good in vitro inhibitory activities against both Drosophila melanogaster acetylcholinesterase (DmAChE) and Musca domestica acetylcholinesterase (MdAChE). Among them, compound I (n = 7) was found to be most potent AChE inhibitor (IC50 = 8.07 μM to DmAChE, IC50 = 32.24 μM to MdAChE), whose activities were 2.31- and 1.35-fold more active than the pos. control ethion (CP, IC50 = 18.62 μM to DmAChE, IC50 = 43.56 μM to MdAChE). The docking model study revealed that compound I (n = 7) possessed fitted spatial structure and bound to central pocket and peripheral site of DmAChE. Moreover, most of the compounds I demonstrated high insecticidal activity to Lipaphis erysimi and Tetranychus cinnabarinus at concentration of 300 mg/L. The experimental process involved the reaction of 2-(2-Bromoethyl)isoindoline-1,3-dione(cas: 574-98-1).Quality Control of 2-(2-Bromoethyl)isoindoline-1,3-dione

The Article related to triazolyl isoindoline dione preparation insecticide acetylcholinesterase inhibitor mol docking, acetylcholinesterase, acetylcholinesterase inhibiting potency, dual binding site, heterodimer, insecticidal activity and other aspects.Quality Control of 2-(2-Bromoethyl)isoindoline-1,3-dione

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary