Category: 17201-43-3

Qhobosheane, Malikotsi A.; Beteck, Richard M.; Baratte, Blandine; Robert, Thomas; Ruchaud, Sandrine; Bach, Stephane; Legoabe, Lesetja J. published their research in Chemico-Biological Interactions in 2021. The article was titled 《Exploration of 7-azaindole-coumaranone hybrids and their analogues as protein kinase inhibitors》.Application of 17201-43-3 The article contains the following contents:

7-Azaindole has been labeled a privileged scaffold for the design of new potent inhibitors of protein kinases. In this paper, we determined the inhibition profiles of novel mono- and disubstituted derivatives of 7-azaindole-coumaranone hybrids on various disease-related protein kinases. Eight hit compounds were identified, including a potent Haspin inhibitor with an IC50 value of 0.15 μM. An interesting observation was that all active monosubstituted compounds displayed dual inhibition for Haspin and GSK-3β, while disubstituted derivatives inhibited GSK-3β and LmCK1 from Leishmania major parasite. Analyses of structure activity relationships (SARs) also revealed that mono-substitution with para-fluorobenzyloxy ring produced an equipotent inhibition of Haspin and GSK-3β. Haspin and GSK-3β are relevant targets for developing new anticancer agents while LmCK1 is an innovative target for leishmanicidal drugs. Novel compounds reported in this paper constitute promising starting points for the development of new anticancer and leishmanicidal drugs. The experimental part of the paper was very detailed, including the reaction process of 4-Cyanobenzyl bromide(cas: 17201-43-3Application of 17201-43-3)

4-Cyanobenzyl bromide(cas: 17201-43-3) is used in the synthesis of ligands containing a chelating pyrazolyl-pyridine group with a pendant aromatic nitrile. It is also useful in the preparation of 4-[(2H-tetra-zol-2-yl)methyl]benzonitrile by reaction with 2H-tetrazole in the presence of potassium hydroxide.Application of 17201-43-3

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Petritsch, Markus; Seebacher, Werner; Mohsin, Noor-ul-Amin; Dolensky, Johanna; Hochegger, Patrick; Kaiser, Marcel; Maeser, Pascal; Belaj, Ferdinand; Saf, Robert; Kretschmer, Nadine; Alajlani, Muaaz; Brantner, Adelheid; Bauer, Rudolf; Schuehly, Wolfgang; Weis, Robert published their research in European Journal of Medicinal Chemistry in 2021. The article was titled 《Preparation of new 1,3-dibenzyl tetrahydropyridinylidene ammonium salts and their antimicrobial and anticellular activities》.SDS of cas: 17201-43-3 The article contains the following contents:

New 1,3 dibenzyl -tetrahydropyridinylidene ammonium salts I [R1R2 = -(CH2)4-, -(CH2)5-; R3 = Ph, 4-chlorophenyl, 2,6-dichlorophenyl, etc.; R4 = Ph, 4-chlorophenyl, 2,6-dichlorophenyl, etc.] were prepared from unsubstituted or N-benzylated tetrahydropyridinylidene ammonium salts II and III. The antiplasmodial and antitrypanosomal activities as well as their cytotoxic effects were determined using microplate assays. In addition, their activities against two gram pos. and two gram neg. bacteria strains and a yeast strain were examined Furthermore, anticancer effects against two cell lines were investigated. Physicochem. parameters were calculated and structure-activity-relationships discussed. One compound showed antiplasmodial activity against a multiresistant strain of Plasmodium falciparum in subnanomolar concentration Antitrypanosomal activities were detected in low nanomolar concentrations A single compound was active against gram pos. and gram neg. bacteria, as well as yeast. One compound inhibited the growth of a HCT cell line in low concentration In the experiment, the researchers used many compounds, for example, 4-Cyanobenzyl bromide(cas: 17201-43-3SDS of cas: 17201-43-3)

4-Cyanobenzyl bromide(cas: 17201-43-3) is a white solid. Its melting point is 113-117°C, and flash point is 125.1°C. It is insoluble in water at 20°C. It is stable under normal temperatures and pressures. It should be stored at 0-5°C.SDS of cas: 17201-43-3

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Nitrile – Wikipedia,
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Thevenin, Marion; Chen, Gang; Kantham, Srinivas; Sun, Chunxiang; Glogauer, Michael; Young, Robert N. published their research in ACS Pharmacology & Translational Science in 2021. The article was titled 《Design, Synthesis, Pharmacokinetics, and Biodistribution of a Series of Bone-Targeting EP4 Receptor Agonist Prodrugs for Treatment of Osteoporosis and Other Bone Conditions》.Application of 17201-43-3 The article contains the following contents:

A series of bone-targeting EP4 receptor agonist conjugate prodrugs were prepared wherein a potent EP4 receptor agonist was bound to a biol. inactive, bisphosphonate-based bone-targeting moiety. Singly and doubly radiolabeled conjugates were synthesized and were shown to be stable in blood, to be rapidly eliminated from the bloodstream, and to be effectively taken up into bone in vivo after i.v. dosing. From these preliminary studies a preferred conjugate 4 (I)(also known as C3 and Mes-1007) was selected for follow up biodistribution and elimination studies. Doubly radiolabeled conjugate 4 was found to partition largely to the liver and bones, and both labels were eliminated from liver at the same rate indicating the conjugate was eliminated intact. Quantification of the labels in bones indicated that free EP4 agonist (EP4a)(2a) was released from bone-bound 4 with a half-time of about 7 days. When dosed orally, radiolabeled 4 was not absorbed and passed through the gastrointestinal tract essentially unchanged, and only traces of radiolabeled 4 were found in the liver, blood, or bones. 4 was found to bind rapidly and completely to powd. bone mineral or to various forms of calcium phosphate, forming a stable matrix suitable for implant and that could made into powders or solid forms and be sterilized without decomposition or release of 4. Basic hydrolysis released free EP4 agonist 2a (II) quant. from the material. In the experimental materials used by the author, we found 4-Cyanobenzyl bromide(cas: 17201-43-3Application of 17201-43-3)

4-Cyanobenzyl bromide(cas: 17201-43-3) is a white solid. Its melting point is 113-117°C, and flash point is 125.1°C. It is insoluble in water at 20°C. It is stable under normal temperatures and pressures. It should be stored at 0-5°C.Application of 17201-43-3

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Nitrile – Wikipedia,
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Formula: C8H6BrNIn 2021 ,《Synthesis and pharmacological evaluation of novel resorcinol biphenyl ether analogs as small molecule inhibitors of PD-1/PD-L1 with benign toxicity profiles for cancer treatment》 appeared in Biochemical Pharmacology (Amsterdam, Netherlands). The author of the article were Cao, Hao; Cheng, Binbin; Liu, Ting; Chen, Jianjun. The article conveys some information:

Programmed death protein 1 (PD-1)/programmed death protein ligand 1 (PD-L1) pathway is one of the most actively pursued targets in cancer immunotherapy. In a continuation of authors research interest in this pathway, synthesized and evaluated the pharmacol. activities of a series of resorcinol biphenyl ether analogs as small mol. PD-1/PD-L1 inhibitors for cancer treatment. Among the 27 newly synthesized compounds, I was found to have the highest inhibitory effect against PD-1/PDL-1 with an IC50 value of 56.58 nM in the HTRF (homogeneous time-resolved fluorescence) assay. In addition, I dose-dependently promoted HepG2 cell death in a co-culture model of HepG2/hPD-L1 and Jurkat T cells. Furthermore, mol. modeling study indicated that I binds with high affinity to the binding interface of PD-L1. Moreover, I effectively inhibited tumor growth (TGI of 76.4% at 90 mg/kg) in an immune checkpoint humanized mouse model with no obvious toxicity. Finally, I did not cause in vivo cardiotoxicity and bone marrow suppression (myelosuppression) to BALB/c mice. Taken together, these results suggest that I deserves further investigation as a potent and safe PD-1/PDL-1 inhibitor for cancer treatment. In the part of experimental materials, we found many familiar compounds, such as 4-Cyanobenzyl bromide(cas: 17201-43-3Formula: C8H6BrN)

4-Cyanobenzyl bromide(cas: 17201-43-3) can reacts with 2H-tetrazole in the presence of KOH to yield 4-[(2H-tetra-zol-2-yl)methyl]benzonitrile. And it may be used in the synthesis of ligands containing a chelating pyrazolyl-pyridine group with a pendant aromatic nitrile.Formula: C8H6BrN

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Nitrile – Wikipedia,
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In 2019,Journal of Materials Chemistry C: Materials for Optical and Electronic Devices included an article by Szukalski, Adam; Moffa, Maria; Camposeo, Andrea; Pisignano, Dario; Mysliwiec, Jaroslaw. Product Details of 17201-43-3. The article was titled 《All-optical switching in dye-doped DNA nanofibers》. The information in the text is summarized as follows:

All-optical switches are introduced which are based on DNA (DNA) in the form of electrospun fibers, where DNA is semi-intercalated with a push-pull, luminescent nonlinear pyrazoline derivative Optical birefringence is found in the organic nanofibers, with fully reversible switching controlled through continuous-wave laser irradiation The photoinduced signal is remarkably large, with birefringence highlighted by optically-driven refractive index anisotropy approaching 0.001. Sub-millisecond characteristic switching times are found. Integrating dye-intercalated DNA complex systems in organic nanofibers, as a convenient and efficient approach to template mol. organization and control it by external stimuli, might open new routes for realizing optical logic gates, reconfigurable photonic networks and sensors through phys.-transient biopolymer components.4-Cyanobenzyl bromide(cas: 17201-43-3Product Details of 17201-43-3) was used in this study.

4-Cyanobenzyl bromide(cas: 17201-43-3) is a white solid. Its melting point is 113-117°C, and flash point is 125.1°C. It is insoluble in water at 20°C. It is stable under normal temperatures and pressures. It should be stored at 0-5°C.Product Details of 17201-43-3

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Nitrile – Wikipedia,
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The author of 《Synthesis of 1,3,4-oxadiazole and imidazo[1,2-a]pyridine based molecular hybrids and their in vitro antituberculosis and cytotoxicity studies》 were Maurya, Shiv Shyam; Gosain, Tannu Priya; Kidwai, Saqib; Singh, Ramandeep; Rawat, Diwan S.. And the article was published in Indian Journal of Chemistry, Section B: Organic Chemistry Including Medicinal Chemistry in 2019. Recommanded Product: 4-Cyanobenzyl bromide The author mentioned the following in the article:

A library of novel 1,3,4-oxadiazole substituted imidazo[1,2-a]pyridine based mol. hybrids I (R = Br, Cl, Me; R1 = 2-nitrobenzyl, naphthalen-1-ylmethyl, (E)-geranyl, etc.) have been synthesized and evaluated against mycobacterium tuberculosis H37Rv. Out of 59 compounds synthesized, ten compounds show activity in the range of 3.125-12.5 μM. Compound I (R = Br, R1 = hexyl) is found to be most active with MIC99 value of 3.125-6.25 μM. Further, these ten compounds have also been tested for their toxicity against THP-1 cell line and are found to be non-toxic with TC50 value in the range of (10 – >50 μM) concentration The results came from multiple reactions, including the reaction of 4-Cyanobenzyl bromide(cas: 17201-43-3Recommanded Product: 4-Cyanobenzyl bromide)

4-Cyanobenzyl bromide(cas: 17201-43-3) is a white solid. Its melting point is 113-117°C, and flash point is 125.1°C. It is insoluble in water at 20°C. It is stable under normal temperatures and pressures. It should be stored at 0-5°C.Recommanded Product: 4-Cyanobenzyl bromide

Referemce:
Nitrile – Wikipedia,
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The author of 《Molecular hybridization approach for phenothiazine incorporated 1,2,3-triazole hybrids as promising antimicrobial agents: Design, synthesis, molecular docking and in silico ADME studies》 were Reddyrajula, Rajkumar; Dalimba, Udayakumar; Madan Kumar, S.. And the article was published in European Journal of Medicinal Chemistry in 2019. Reference of 4-Cyanobenzyl bromide The author mentioned the following in the article:

The synthesis a library consisting of four sets of phenothiazine incorporated 1,2,3-triazole compounds using mol. hybridization approach. The new hybrid mols. were synthesized and screened for in-vitro growth inhibition activity against Mycobacterium tuberculosis H37Rv strain (ATCC-27294). Among the tested compounds, nineteen compounds exhibited significant activity with MIC value 1.6 μg/mL, which was two fold higher than the MIC value of standard first-line TB drug Pyrazinamide. In addition, all these compounds were proved to be non-toxic (with selective index > 40) against VERO cell lines. However, these compounds did not inhibit significantly the growth of Staphylococcus aureus, Escherichia coli and Pseudomonas aeruginosa strains: the activity profile was similar to that observed for standard anti-TB drugs (isoniazid and pyrazinamide), indicating the specificity of these compounds towards the Mycobacterium tuberculosis strain. The mol. docking studies against two target enzymes (Inh A and CYP121) to further validate the antitubercular potency of these mols. was reported. Furthermore, prediction of in silico-ADME and pharmacokinetic parameters indicated that these compounds were good oral bioavailability. The results suggested that these phenothiazine incorporated 1,2,3-triazole compounds were a promising class of mol. entities for the development of new antitubercular leads.4-Cyanobenzyl bromide(cas: 17201-43-3Reference of 4-Cyanobenzyl bromide) was used in this study.

4-Cyanobenzyl bromide(cas: 17201-43-3) is an important intermediate for pharmaceutical production. It can be used for the synthesis of a series of piperidine-linked aromatic diimidazolines, which have been synthesized as conformationally restricted congeners of the anti-Pneumocystis carinii (PCP) drug, Pentamidine.Reference of 4-Cyanobenzyl bromide

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《Design, synthesis, biological evaluation and molecular docking of new uracil analogs-1,2,4-oxadiazole hybrids as potential anticancer agents》 was written by El Mansouri, Az-Eddine; Oubella, Ali; Maatallah, Mohamed; AitItto, Moulay Youssef; Zahouily, Mohamed; Morjani, Hamid; Lazrek, Hassan B.. Recommanded Product: 4-Cyanobenzyl bromideThis research focused onuracil oxadiazole hybrid preparation caspase mol docking anticancer agent; 1,2,4-Oxadiazole; Anticancer activity; Apoptosis; Heterogeneous catalyst; Hybrid molecules; Molecular docking; Uracil analogues. The article conveys some information:

A new series of uracil analogs-1,2,4-oxadiazole hybrid derivatives were synthesized by a new, simple, and efficient method using for the first time HAP-SO3H as an heterogeneous acid catalyst for the condensation and cyclization between amidoxime and aldehyde. The new derivatives were characterized by HRMS, FTIR, 1H NMR, and 13C NMR spectroscopy techniques. The synthesized 1,2,4-oxadiazole hybrids were evaluated for their cytotoxic activity in five human cancer cell lines: melanoma (A-375), fibrosarcoma (HT-1080), breast (MCF-7 and MDA-MB-231), and lung carcinoma (A-549). Compounds 1-[4-(5-Biphenyl-4-yl-[1,2,4]oxadiazol-3-yl)-benzyl]-5-fluoro-1H-pyrimidine-2,4-dione and 5-Fluoro-1-{4-[5-(4′-methoxy-biphenyl-4-yl)-[1,2,4]oxadiazol-3-yl]-benzyl}-1H-pyrimidine-2,4-dione were potent cytotoxic agents against HT-1080 and MFC-7 cells with IC50 inferior to 1μM. The possible mechanism of apoptosis induction by the derivatives was studied using Annexin v staining, caspase-3/7 activity, mitochondrial membrane potential measurement, and anal. cell cycle progression. The compound 1-[4-(5-Biphenyl-4-yl-[1,2,4]oxadiazol-3-yl)-benzyl]-5-fluoro-1H-pyrimidine-2,4-dione induced apoptosis through caspase-3/7 activation and S-phase arrest in HT-1080 and A549 cells. The mol. docking showed that compound 1-[4-(5-Biphenyl-4-yl-[1,2,4]oxadiazol-3-yl)-benzyl]-5-fluoro-1H-pyrimidine-2,4-dione activated the caspase-3 by forming a stable protein-ligand complex. In the experiment, the researchers used many compounds, for example, 4-Cyanobenzyl bromide(cas: 17201-43-3Recommanded Product: 4-Cyanobenzyl bromide)

4-Cyanobenzyl bromide(cas: 17201-43-3) can reacts with 2H-tetrazole in the presence of KOH to yield 4-[(2H-tetra-zol-2-yl)methyl]benzonitrile. And it may be used in the synthesis of ligands containing a chelating pyrazolyl-pyridine group with a pendant aromatic nitrile.Recommanded Product: 4-Cyanobenzyl bromide

Referemce:
Nitrile – Wikipedia,
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《Synthesis of difluoromethyl and deuterium-labeled difluoromethyl thioethers from aliphatic electrophiles》 was published in Chemical Communications (Cambridge, United Kingdom) in 2020. These research results belong to Ding, Tianqi; Jiang, Lvqi; Yi, Wenbin. SDS of cas: 17201-43-3 The article mentions the following:

A one-pot difluoromethylthiolation of alkyl electrophiles with thiourea and di-Et bromodifluoromethylphosphonate is described. The transition-metal-free approach, readily available reagents, and mild conditions provide a practical way for the synthesis of difluoromethyl thioethers. By changing the “”H”” source to the most commonly used “”D”” sources CD3OD and D2O, this strategy enables efficient synthesis of SCF2D-substituted mols. in good yields with high levels of D incorporation. In addition to this study using 4-Cyanobenzyl bromide, there are many other studies that have used 4-Cyanobenzyl bromide(cas: 17201-43-3SDS of cas: 17201-43-3) was used in this study.

4-Cyanobenzyl bromide(cas: 17201-43-3) is a white solid. Its melting point is 113-117°C, and flash point is 125.1°C. It is insoluble in water at 20°C. It is stable under normal temperatures and pressures. It should be stored at 0-5°C.SDS of cas: 17201-43-3

Referemce:
Nitrile – Wikipedia,
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Yang, Ren-Yin; Wang, Hui; Xu, Bo published their research in Chemical Communications (Cambridge, United Kingdom) in 2021. The article was titled 《Base promoted gem-difluoroolefination of alkyl triflones》.Recommanded Product: 4-Cyanobenzyl bromide The article contains the following contents:

A new synthesis of gem-difluoroalkenes ArC(R)=CF2 [Ar = 4-bromophenyl, naphthalen-2-yl, 5-(methoxycarbonyl)thiophen-2-yl, etc.; R = prop-2-en-1-yl, 3-phenylprop-2-yn-1-yl, (4-methylphenyl)methyl, etc.] from readily available alkyl triflones ArCH(R)S(O)2CF3 and difluorocarbene precursors such as TMSCF2Br has been reported. The reaction, regardless of electronic effect, gives gem-difluoroalkenes ArC(R)=CF2 in good to excellent yields. The mechanism may involve deprotonation of triflones, nucleophilic addition, and the elimination of SO2CF3. In the experiment, the researchers used 4-Cyanobenzyl bromide(cas: 17201-43-3Recommanded Product: 4-Cyanobenzyl bromide)

4-Cyanobenzyl bromide(cas: 17201-43-3) is a white solid. Its melting point is 113-117°C, and flash point is 125.1°C. It is insoluble in water at 20°C. It is stable under normal temperatures and pressures. It should be stored at 0-5°C.Recommanded Product: 4-Cyanobenzyl bromide

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts