Author: Jessica.F

Saul, Sirle published the artcileIdentification and evaluation of 4-anilinoquin(az)olines as potent inhibitors of both dengue virus (DENV) and Venezuelan equine encephalitis virus (VEEV), Safety of 2-Aminobenzonitrile(Flakes or Chunks), the main research area is anilinoquinoline anilinoquinazoline antiviral dengue virus Venezuelan equine encephalitis virus; Alphavirus; Antiviral; Dengue virus; Flavivirus; Venezuelan equine encephalitis virus.

There is an urgent need for novel strategies for the treatment of emerging arthropod-borne viral infections, including those caused by dengue virus (DENV) and Venezuelan equine encephalitis virus (VEEV). We prepared and screened focused libraries of 4-anilinoquinolines and 4-anilinoquinazolines for antiviral activity and identified three potent compounds N-(2,5-dimethoxyphenyl)-6-(trifluoromethyl)quinolin-4-amine (10, I) inhibited DENV infection with an EC50 = 0.25μM, N-(3,4-dichlorophenyl)-6-(trifluoromethyl)quinolin-4-amine (27, II) inhibited VEEV with an EC50 = 0.50μM, while N-(3-ethynyl-4-fluorophenyl)-6,7-dimethoxyquinazolin-4-amine (54, III) inhibited VEEV with an EC50 = 0.60μM. These series of compounds demonstrated nearly no toxicity with CC50 values greater than 10μM in all cases. These promising results provide a future prospective to develop a clin. compound against these emerging viral threats.

Bioorganic & Medicinal Chemistry Letters published new progress about Antiviral agents. 1885-29-6 belongs to class nitriles-buliding-blocks, name is 2-Aminobenzonitrile(Flakes or Chunks), and the molecular formula is C7H6N2, Safety of 2-Aminobenzonitrile(Flakes or Chunks).

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

Hwu, Jih Ru published the artcileSynthesis and antiviral activities of quinazolinamine-coumarin conjugates toward chikungunya and hepatitis C viruses, HPLC of Formula: 1885-29-6, the main research area is quinazolinamine coumarin preparation antiviral chikungunya hepatitis C virus; Broad-spectrum; Chikungunya virus; Coumarin; Hepatitis C virus; Quinazolin-4-amine; Structure–activity relationship.

Development of new drugs with broad-spectrum to combat RNA viruses would be beneficial to mankind but faces a great challenge. Authors designed and efficiently synthesized a series of quinazolin-4-amine-SCH2-coumarin conjugated compounds Authors data of the virus-cell-based assay show five new conjugates inhibit chikungunya virus with EC50 values as potent as 1.96μM and two conjugates inhibit hepatitis C virus with EC50 values as low as 16.6μM. These conjugates possess a xylene substituent at the C-4 amino group of quinazoline and a t-Bu substituent at the C-6′ position of coumarin.

European Journal of Medicinal Chemistry published new progress about Antiviral agents. 1885-29-6 belongs to class nitriles-buliding-blocks, name is 2-Aminobenzonitrile(Flakes or Chunks), and the molecular formula is C7H6N2, HPLC of Formula: 1885-29-6.

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

White, Kris published the artcileAryl Sulfonamide Inhibits Entry and Replication of Diverse Influenza Viruses via the Hemagglutinin Protein, Application of 2-Aminobenzonitrile(Flakes or Chunks), the main research area is aryl sulfonamide preparation influenza virus entry replication hemagglutinin.

Influenza viruses cause approx. half a million deaths every year worldwide. Vaccines are available but partially effective, and the number of antiviral medications is limited. Thus, it is crucial to develop therapeutic strategies to counteract this major pathogen. Influenza viruses enter the host cell via their hemagglutinin (HA) proteins. The HA subtypes of influenza A virus are phylogenetically classified into groups 1 and 2. Here, we identified an inhibitor of the HA protein, a tertiary aryl sulfonamide, that prevents influenza virus entry and replication. This compound shows potent antiviral activity against diverse H1N1, H5N1, and H3N2 influenza viruses encoding HA proteins from both groups 1 and 2. Synthesis of derivatives of this aryl sulfonamide identified moieties important for antiviral activity. This compound may be considered as a lead for drug development with the intent to be used alone or in combination with other influenza A virus antivirals to enhance pan-subtype efficacy.

Journal of Medicinal Chemistry published new progress about Antiviral agents. 1885-29-6 belongs to class nitriles-buliding-blocks, name is 2-Aminobenzonitrile(Flakes or Chunks), and the molecular formula is C7H6N2, Application of 2-Aminobenzonitrile(Flakes or Chunks).

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

Biyiklioglu, Mack published the artcilePi-stacking interaction perphenazine modified zinc(II) phthalocyanine nanoparticles for photothermal and photodynamic therapy, Quality Control of 91-15-6, the main research area is perphenazine zinc phthalocyanine nanoparticle photothermal photodynamic therapy.

Photodynamic therapy and photothermal therapy as non-invasive treatment methods have been receiving more and more attention. The report shows that zinc(II) phthalocyanine (Pc2) modified by perphenazine forms nanoparticles with a particle size of 110 nm by π-π stacking in water. It has good photothermal effect when illuminated by 680 nm laser in aqueous solution In addition, its ability to produce active oxygen is 2.3-fold that of methylene blue, so Pc2 also has a good photodynamic effect. In vivo fluorescence shows that Pc2 has a good targeting effect on tumors. Under the synergistic effect of photodynamic therapy and photothermal therapy, Pc2 has good tumor inhibition efficiency.

Journal of Porphyrins and Phthalocyanines published new progress about Antitumor agents. 91-15-6 belongs to class nitriles-buliding-blocks, name is Phthalonitrile, and the molecular formula is C8H4N2, Quality Control of 91-15-6.

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

Ekineker, Gulcin published the artcileNewly axially silicon (IV) phthalocyanine photosensitizer: design, synthesis and photo-chemical properties, HPLC of Formula: 91-15-6, the main research area is silicon phthalocyanine photosensitizer design synthesis photochem property.

Phthalocyanines as used a photosensitizer in photodynamic therapy, phthalocyanines exhibit their long wavelength absorption and the ability to produce high singlet oxygen for tumor destruction with 650 to 900 nm fluorescence. In this study, new axially substituted silicon (IV) phthalocyanine (PS-4) was synthesized to determine photo-chem. properties using 2-methoxyethanol as an axial ligand to increase singlet oxygen quantum yield. Structural characterization of this new axially substituted silicon (IV) phthalocyanine were performed by IR, mass, 1H NMR and UV-Vis spectroscopic techniques. As axially substituted silicon (IV) phthalocyanine (PS-4) is thought to be a promising PDT agent, photo-chem. properties for cancer treatment with PDT have been investigated.

CBU Journal of Science published new progress about Antitumor agents. 91-15-6 belongs to class nitriles-buliding-blocks, name is Phthalonitrile, and the molecular formula is C8H4N2, HPLC of Formula: 91-15-6.

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

Oekchuae, Sittisak published the artcileThe Design and Synthesis of a New Series of 1,2,3-Triazole-Cored Structures Tethering Aryl Urea and Their Highly Selective Cytotoxicity toward HepG2, Recommanded Product: 2-Aminobenzonitrile(Flakes or Chunks), the main research area is triazole cored aryl urea preparation antitumor human; 1,2,3-triazole-containing drug; click reaction; drug discovery; hepatocellular carcinoma (HCC); selective anti-HepG2 agent; sorafenib analog; targeted cancer drug.

Herein, a new series of 1,2,3-triazole-cored structures incorporating aryl urea I [R = H, 2-Me, 4-F, etc.] as anti-HepG2 agents was designed and synthesized via nucleophilic addition and copper-catalyzed azide-alkyne cycloaddition (CuAAC) with excellent yields. Significantly, almost all triazole-cored analogs exhibited less cytotoxicity toward normal cells, human embryonal lung fibroblast cell MRC-5, compared to Sorafenib and Doxorubicin. Among them, I [R = 2-OEt, 2-Cl] exhibited the highest selectivity indexes (SI = 14.7 and 12.2), which were ca. 4.4- and 3.7-fold superior to that of Sorafenib (SI = 3.30) and ca. 3.8- and 3.2-fold superior to that of Doxorubicin (SI = 3.83), resp. Addnl., excellent inhibitory activity against hepatocellular carcinoma HepG2, comparable to Sorafenib, was still maintained. A cell-cycle anal. and apoptosis induction study suggested that I [R = 2-OEt, 2-Cl] likely share a similar mechanism of action to Sorafenib. Furthermore, compounds I [R = 2-OEt, 2-Cl] exhibit appropriate drug-likeness, analyzed by SwissADME. With their excellent anti-HepG2 activity, improved selectivity indexes, and appropriate druggability, the triazole-cored analogs I [R = 2-OEt, 2-Cl] are suggested to be promising candidates for development as targeted cancer agents and drugs used in combination therapy for the treatment of HCC.

Pharmaceuticals published new progress about Antitumor agents. 1885-29-6 belongs to class nitriles-buliding-blocks, name is 2-Aminobenzonitrile(Flakes or Chunks), and the molecular formula is C7H6N2, Recommanded Product: 2-Aminobenzonitrile(Flakes or Chunks).

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

Li, Shuai published the artcileDesign, synthesis and biological evaluation of erythrina derivatives bearing a 1,2,3-triazole moiety as PARP-1 inhibitors, Recommanded Product: 2-Aminobenzonitrile(Flakes or Chunks), the main research area is erythrina triazole preparation PARP 1 inhibitor antitumor structure activity; 1,2,3-Triazole; Apoptosis; Erythrina; PARP-1 inhibitor.

Inhibitors of poly (ADP-ribose) polymerase-1 (PARP-1) have shown to be promising in clin. trials against cancer, and many researchers are interested in the development of new PARP-1 inhibitors. Herein, we designed and synthesized 44 novel erythrina derivatives bearing a 1,2,3-triazole moiety, I (RR1 = O, R2 = H, 2-Me, 3-MeO, 4-Me, etc.; R = OH, R1 = H), as PARP-1 inhibitors. MTT assay results indicated that compound I (RR1 = O, R2 = 2-F) (II) had the most potent anti-proliferative activity against A549 cells among five cancer cells. The enzyme inhibitory activity in vitro of compound II was also significantly better than rucaparib. Furthermore, the selectivity index of compound II was higher than rucaparib for lung cancer cells. Flow cytometry anal. showed that compound II induced apoptosis of A549 cells by the mitochondrial pathway. Western blot anal. indicated that compound II was able to inhibit the biosynthesis of PAR effectively, and it was more potent than rucaparib. Also, compound II was able to up-regulate the ratio of bax/bcl-2, activate caspase-3, and ultimately induced apoptosis of A549 cells. The combined results revealed that the discovery of novel non-amide based PARP-1 inhibitors have great research significance and provide a better choice for the future development of drugs.

Bioorganic Chemistry published new progress about Antitumor agents. 1885-29-6 belongs to class nitriles-buliding-blocks, name is 2-Aminobenzonitrile(Flakes or Chunks), and the molecular formula is C7H6N2, Recommanded Product: 2-Aminobenzonitrile(Flakes or Chunks).

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

Zhao, Xuan published the artcileA monoamine oxidase-A inhibitor phthalocyanine conjugate for targeted photodynamic therapy and inhibition of prostate cancer metastasis in vitro, Recommanded Product: Phthalonitrile, the main research area is preparation MAOA inhibitor phthalocyanine conjugate prostate cancer metastasis PDT.

Photodynamic therapy (PDT), as an alternative non-invasive clin. treatment modality, has been extensively employed for various anticancer applications in preclin. and clin. trials. However, there is hardly any PDT research based on invasive or metastatic tumors. But it can′t be ignored that cancer metastases are responsible for 90% of all cancer-related death. Among these metastatic cancers, prostate cancer (PCa) is regarded as one of the leading causes of cancer related deaths amongst male patients due to its high metastasis and high fatality rate. At present, it remains a great challenge to apply traditional PDT technol. for inhibiting prostate cancer metastasis. In this work, we successfully designed and synthesized a novel MAO-A targeted photosensitizer Pc-MLB for targeted photodynamic treatment of prostate cancer and inhibiting its metastasis in vitro. In vitro experiments demonstrate that Pc-MLB shows high target affinity and specificity towards prostate cancer cells and remarkable photodynamic anticancer activity compared with the control. More significantly, the migration and invasion assays show that Pc-MLB exhibits the ability to inhibit the migration and metastasis of prostate cancer cells to some extent.

Dyes and Pigments published new progress about Antitumor agents. 91-15-6 belongs to class nitriles-buliding-blocks, name is Phthalonitrile, and the molecular formula is C8H4N2, Recommanded Product: Phthalonitrile.

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

Ertas, Merve published the artcilePotent ribonucleotide reductase inhibitors: Thiazole-containing thiosemicarbazone derivatives, HPLC of Formula: 100-70-9, the main research area is antitumor agents ribonucleotide reductase inhibitors thiazole thiosemicarbazone ADME; antitumor agents; ribonucleotide reductase; thiazole; thiosemicarbazone.

The antioxidant, antimalarial, antibacterial, and antitumor activities of thiosemicarbazones have made this class of compounds important for medicinal chemists. In addition, thiosemicarbazones are among the most potent and well-known ribonucleotide reductase inhibitors. In this study, 24 new thiosemicarbazone derivatives were synthesized, and the structures and purity of the compounds were determined by IR, 1H NMR, 13C NMR, mass spectroscopy, and elemental anal. The IC50 values of these 24 compounds were determined with an assay for ribonucleotide reductase inhibition. Compounds 19, 20, and 24 inhibited ribonucleotide reductase enzyme activity at a higher level than metisazone as standard The cytotoxic effects of these compounds were measured on the MCF7 (human breast adenocarcinoma) and HEK293 (human embryonic kidney) cell lines. Similarly, compounds 19, 20, and 24 had a selective effect on the MCF7 and HEK293 cell lines, killing more cancer cells than cisplatin as standard The compounds (especially 19, 20, and 24 as the most active ones) were then subjected to docking experiments to identify the probable interactions between the ligands and the enzyme active site. The complex formation was shown qual. The ADME (absorption, distribution, metabolism, and excretion) properties of the compounds were analyzed using in-silico techniques.

Archiv der Pharmazie (Weinheim, Germany) published new progress about Antitumor agents. 100-70-9 belongs to class nitriles-buliding-blocks, name is Picolinonitrile, and the molecular formula is C6H4N2, HPLC of Formula: 100-70-9.

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

Girgis, Nabih S. published the artcilePhosphorus pentoxide in organic synthesis. VII. Synthesis of 3-aryl-3,7-dihydro-4H-pyrrolo[2,3-d]pyrimidin-4-imines, Application of 2-Amino-4-methyl-1H-pyrrole-3-carbonitrile, the main research area is pyrrolopyrimidinimine aryl preparation antineoplastic; phosphorus pentoxide cyclization acetylaminopyrrolecarbonitrile; pyrrolecarbonitrile acetylamino phosphorus pentoxide cyclization; arylpyrrolopyrimidinimine preparation antineoplastic; fungicide arylpyrrolopyrimidinimine preparation; insecticide arylpyrrolopyrimidinimine preparation; plant regulator arylpyrrolopyrimidinimine preparation; pyrimidinimine arylpyrrolo antineoplastic preparation.

Anhydrous RR1C6H3NH2.HCl (R = H, R1 = H, 4-Cl, 2-F, 4-F, 3-Me, 4-Me, 4-Et, 4-Bu; R = 2-Cl, R1 = 4-Cl; R = 2-Me, R1 = 4-Me) reacted with pyrroles I [R2 = H, CHMeEt, CH2Ph; R3 = Me, Ph), P2O5, and N,N-dimethylcyclohexylamine at 150-180° to give the title compounds II, which were inactive against P388 lymphocytic leukemia. However, II (R = R1 = R2 = H, R3 = Me) was active against the plant louse, II (R = R2 = H, R1 = 4-F, R3 = Ph) was a plant regulator, and II (R = H, R1 = F, R2 = CHMeEt, R3 = Me) was a fungicide against Cercospora on peanut at 200 ppm.

Liebigs Annalen der Chemie published new progress about Antitumor agents. 59146-60-0 belongs to class nitriles-buliding-blocks, name is 2-Amino-4-methyl-1H-pyrrole-3-carbonitrile, and the molecular formula is C6H7N3, Application of 2-Amino-4-methyl-1H-pyrrole-3-carbonitrile.

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts