Month: November 2022

Arber, N. published the artcileSporadic adenomatous polyp regression with exisulind is effective but toxic: a randomized, double blind, placebo controlled, dose-response study, COA of Formula: C20H17FO4S, the publication is Gut (2006), 55(3), 367-373, database is CAplus and MEDLINE.

Background and aim: A 12 mo, multicenter, randomized, double blind, placebo controlled, phase 3, dose-response study was carried out. Exisulind inhibits tumor growth by induction of apoptosis. The aim of our study was to investigate if exisulind induces regression of sporadic colonic adenomas. Patients and methods: A 12 mo multicenter randomized double blind placebo controlled phase 3 dose response study was carried out. At baseline colonoscopy, left sided polyps (3-10 mm) were tattooed, measured, and left in place. Subjects received exisulind 200 or 400 mg, or placebo daily. Follow up sigmoidoscopy was performed after six months, and removal of any remaining polyps at the 12 mo colonoscopy. The primary efficacy variable was change in polyp size from baseline. Results: A total of 281 patients were enrolled and randomized; 155 (55%) fulfilled the criteria for the intention to treat (ITT) anal. and 114 (41%) fulfilled the criteria for the efficacy evaluation anal. (patients who underwent the 12 mo colonoscopy). The decrease in median polyp size was significantly greater (p = 0.03) in patients who received exisulind 400 mg (-10 mm²) compared with those who received placebo (-4 mm²). Complete or partial response was significantly higher in the exisulind 400 mg group (54.6%) compared with the placebo group (30.2%), and disease progression was significantly lower (6.1% v 27.9%) (p = 0.04 and 0.02, resp.). Increased liver enzymes (8.4%) and abdominal pain (14.7%) were also reported at a greater frequency in the exisulind 400 mg group. Conclusion: Exisulind caused significant regression of sporadic adenomatous polyps but was associated with more toxicity. This model of polyp regression, short in its term and involving a comparatively small patient sample size, may be the best available tool to assess a therapeutic regimen before launching into large preventive clin. studies.

Gut published new progress about 59973-80-7. 59973-80-7 belongs to naphthyridine, auxiliary class Immunology/Inflammation,COX, name is Sulindac sulfone, and the molecular formula is C20H17FO4S, COA of Formula: C20H17FO4S.

Referemce:
https://en.wikipedia.org/wiki/1,8-Naphthyridine,
1,8-Naphthyridine | C8H6N2 – PubChem

Thirugnanaselvi, S. published the artcileStructural and biological activities of (4Z)-4-(3-phenyl allylidene amino)-3-hydroxy naphthalene-1-sulfonic acid (AC) and naphthalene-1-yl-thiophene-2-ylmethyleneamine (NT) as Schiff bases, Product Details of C10H9NO4S, the publication is International Journal of Chemical Sciences (2016), 14(2), 559-569, database is CAplus.

Schiff bases (4Z)-4-(3-Ph allylidene amino)-3-hydroxy naphthalene-1-sulfonic acid (AC) and naphthalene-1-yl-thiophene-2-ylmethylene-amine (NT) derived from the condensation reaction of Analar grade 1-amino-2-naphthol 4-sulfonic acid WITH Cinnamaldehyde and naphthalene-1-ylamine and thiophene-2-carboxaldehyde, resp. was prepared The synthesis was carried out under microwave condition. This Schiff base was analyzed by infra-red and UV. The all prepared compounds were assayed for antibacterial (Bacillus subtilis MTCC 441, Staphylococcus aureus MTCC 96, Echirichia coli MTCC 1689 and Proteus vulgaris MTCC 742) and antifungal (Aspergillus sp. and Candida albicans) activities by disk diffusion method. The results indicate that all tested compounds show antibacterial activity against E. coli, as gram pos. and neg. bacteria, and antifungal activity against C. albicans. But the compounds AC having 1-OH and 1-HSO₃ substituted showed good inhibition against bacteria and fungi as compare to standard drugs.

International Journal of Chemical Sciences published new progress about 116-63-2. 116-63-2 belongs to naphthyridine, auxiliary class Sulfonic acid,Amine,Naphthalene,Alcohol,Organic Pigment, name is 4-Amino-3-hydroxynaphthalene-1-sulfonic acid, and the molecular formula is C3H9ClOS, Product Details of C10H9NO4S.

Referemce:
https://en.wikipedia.org/wiki/1,8-Naphthyridine,
1,8-Naphthyridine | C8H6N2 – PubChem

Thirugnanaselvi, S. published the artcileEffect of Schiff base as corrosion inhibitor on AZ31 magnesium alloy in hydrochloric acid solution, Application In Synthesis of 116-63-2, the publication is Transactions of Nonferrous Metals Society of China (2014), 24(6), 1969-1977, database is CAplus.

Schiff base derived from the condensation reaction of analar grade 1-amino-2-naphthol 4-sulfonic acid with cinnamaldehyde was prepared under microwave condition. The Schiff base was analyzed by IR spectroscopy. This Schiff base as a corrosion inhibitor of AZ31 magnesium alloy in 0.05 mol/L HCl solution was studied. The inhibition effect of the Schiff base compound (4Z)-4-(3-Ph allylidene amino)-3-hydroxy naphthalene-1-sulfonic acid (AC) on AZ31 magnesium alloy corrosion was studied using mass loss, potentiodynamic polarization technique, electrochem. impedance spectroscopy methods. The potentiodynamic polarization curve shows that Schiff base AC inhibits both anodic and cathodic reactions at all concentration, which indicates it is a mixed type inhibitor. EIS results indicate that as the additive concentration is increased, the polarization resistance increases whereas double-layer capacitance decreases. The adsorption of AC on the AZ31 magnesium alloy surface in 0.05 mol/L HCl obeys the Langmuir adsorption isotherm.

Transactions of Nonferrous Metals Society of China published new progress about 116-63-2. 116-63-2 belongs to naphthyridine, auxiliary class Sulfonic acid,Amine,Naphthalene,Alcohol,Organic Pigment, name is 4-Amino-3-hydroxynaphthalene-1-sulfonic acid, and the molecular formula is C19H34ClN, Application In Synthesis of 116-63-2.

Referemce:
https://en.wikipedia.org/wiki/1,8-Naphthyridine,
1,8-Naphthyridine | C8H6N2 – PubChem

Frahm, Silke published the artcileSulindac derivatives inhibit cell growth and induce apoptosis in primary cells from malignant peripheral nerve sheath tumors of NF1-patients, HPLC of Formula: 59973-80-7, the publication is Cancer Cell International (2004), No pp. given, database is CAplus.

Background: Malignant peripheral nerve sheath tumors (MPNSTs) are neoplasms leading to death in most cases. Patients with Neurofibromatosis type 1 have an increased risk of developing this malignancy. The metabolites of the inactive prodrug Sulindac, Sulindac Sulfide and Sulindac Sulfone (Exisulind) are new chemopreventive agents that show promising results in the treatment of different cancer types. In this study we examined the antineoplastic effect of these compounds on primary cells derived from two MPNSTs of Neurofibromatosis type 1 patients. Results: Exisulind and Sulindac Sulfide showed a dramatic time- and dose-dependent growth inhibitory effect with IC50-values of 120 渭M, and 63 渭M, resp. The decrease in viability of the tested cells correlated with induction of apoptosis. Treatment with 500 渭M Exisulind and 125 渭M Sulindac Sulfide for a period of 2 days increased the rate of apoptosis 21-27-fold compared to untreated cells. Reduced expression of RAS-GTP and phosphorylated ERK1/2 was detected in treated MPNST cells. Moreover, elevated levels of phosphorylated SAPK/JNK were found after drug treatment, and low activation of cleaved caspase-3 was seen. Conclusions: Our results suggest that this class of compounds may be of therapeutic benefit for Neurofibromatosis type 1 patients with MPNST.

Cancer Cell International published new progress about 59973-80-7. 59973-80-7 belongs to naphthyridine, auxiliary class Immunology/Inflammation,COX, name is Sulindac sulfone, and the molecular formula is C20H17FO4S, HPLC of Formula: 59973-80-7.

Referemce:
https://en.wikipedia.org/wiki/1,8-Naphthyridine,
1,8-Naphthyridine | C8H6N2 – PubChem

Kempe, Hideto published the artcileEnormously extended 蟺-electronic conjugation system of dimeric octaethylporphyrin transmitted with anthracene, Application In Synthesis of 18512-55-5, the publication is Tetrahedron Letters (2014), 55(37), 5164-5169, database is CAplus.

Based on the fact that anthracene (Anth) possesses much higher similarity in electron-releasing ability to porphyrin nucleus than the other polyacenes, the dimeric octaethylporphyrin (OEP) derivatives 4 and 5 (OEP-Anth-OEP) were synthesized and their structure-property relations were examined, as compared with related OEP dimers 1-3. Among them, the derivative 4 showed enormously high electronic communication between two terminal OEP rings, potentially providing a suitable unit of the electronic structure for mol. design of the OEP devices operating with less energy and with higher sensitivity to outside stimuli.

Tetrahedron Letters published new progress about 18512-55-5. 18512-55-5 belongs to naphthyridine, auxiliary class Alkynyl,Anthracene, name is 9,10-Diethynylanthracene, and the molecular formula is C18H10, Application In Synthesis of 18512-55-5.

Referemce:
https://en.wikipedia.org/wiki/1,8-Naphthyridine,
1,8-Naphthyridine | C8H6N2 – PubChem

Dibble, David J. published the artcileAza-Diels-Alder Approach to Diquinolineanthracene and Polydiquinolineanthracene Derivatives, Application of 9,10-Diethynylanthracene, the publication is Organic Letters (2018), 20(3), 502-505, database is CAplus and MEDLINE.

This study describes the synthesis of modular diquinolineanthracene and polydiquinolineanthracene derivatives The reported facile and scalable aza-Diels-Alder-based approach requires mild conditions, proceeds in two steps, uses com. available starting materials, and accommodates varying functionalities. Given the known utility of the acene and quinoline motifs, the synthesized mols. and polymers hold promise for organic electronics applications.

Organic Letters published new progress about 18512-55-5. 18512-55-5 belongs to naphthyridine, auxiliary class Alkynyl,Anthracene, name is 9,10-Diethynylanthracene, and the molecular formula is C18H10, Application of 9,10-Diethynylanthracene.

Referemce:
https://en.wikipedia.org/wiki/1,8-Naphthyridine,
1,8-Naphthyridine | C8H6N2 – PubChem

Kumar, Rajesh published the artcileSynthesis, anti-microbial evaluation, and QSAR studies of 4-amino-3-hydroxy-naphthalene-1-sulfonic acid derivatives, Name: 4-Amino-3-hydroxynaphthalene-1-sulfonic acid, the publication is Medicinal Chemistry Research (2012), 21(12), 4301-4310, database is CAplus.

A series of 4-amino-3-hydroxy-naphthalene-1-sulfonic acid derivatives was synthesized and tested in vitro for its anti-microbial potential. The results of anti-microbial studies indicated that derivatives I [R¹ = H, R² = R³ = R⁴ = OMe; R¹ = R³ = Cl, R² = R⁴ =H] were found to be most effective ones. The mt-QSAR model for anti-microbial activity revealed the importance of topol. parameter, valence zero-order mol. connectivity index (⁰蠂^v) in describing the anti-microbial activity of synthesized 4-amino-3-hydroxy-naphthalene-1-sulfonic acid derivatives

Medicinal Chemistry Research published new progress about 116-63-2. 116-63-2 belongs to naphthyridine, auxiliary class Sulfonic acid,Amine,Naphthalene,Alcohol,Organic Pigment, name is 4-Amino-3-hydroxynaphthalene-1-sulfonic acid, and the molecular formula is C10H9NO4S, Name: 4-Amino-3-hydroxynaphthalene-1-sulfonic acid.

Referemce:
https://en.wikipedia.org/wiki/1,8-Naphthyridine,
1,8-Naphthyridine | C8H6N2 – PubChem

Thomas, Ambily published the artcileCommunication-Electrooxidation of Dopamine at CoNP-pAHNSA Modified Electrode: A Sensitive Approach to Its Determination, Name: 4-Amino-3-hydroxynaphthalene-1-sulfonic acid, the publication is Journal of the Electrochemical Society (2018), 165(10), B466-B468, database is CAplus.

A voltammetric sensor for the simple and rapid determination of dopamine (DA) has been developed using a glassy carbon electrode modified with cobalt nano/poly (4-amino-3-hyroxy-1-naphthalenesulfonic acid) composite. On square wave voltammetric mode, the modified electrode was found to efficiently catalyze the electrochem. oxidation of DA in 0.1 M PBS (pH 7). Response of DA increased linearly with its concentration in the range 5 脳 10^-5 M to 5 脳 10^-7 M with a limit of detection (LOD) 1.75 脳 10^-8 M. Reliability of the developed sensor in real sample anal. was ascertained successfully by determining DA in artificial blood serum, urine and cerebrospinal fluid (CSF).

Journal of the Electrochemical Society published new progress about 116-63-2. 116-63-2 belongs to naphthyridine, auxiliary class Sulfonic acid,Amine,Naphthalene,Alcohol,Organic Pigment, name is 4-Amino-3-hydroxynaphthalene-1-sulfonic acid, and the molecular formula is C2H4ClNO, Name: 4-Amino-3-hydroxynaphthalene-1-sulfonic acid.

Referemce:
https://en.wikipedia.org/wiki/1,8-Naphthyridine,
1,8-Naphthyridine | C8H6N2 – PubChem

Mathew, Manna Rachel published the artcilePoly(amino hydroxy naphthalene sulphonic acid) modified glassy carbon electrode; an effective sensing platform for the simultaneous determination of xanthine and hypoxanthine, Application of 4-Amino-3-hydroxynaphthalene-1-sulfonic acid, the publication is Journal of the Electrochemical Society (2020), 167(4), 047519, database is CAplus.

A rapid, simple and reliable electrochem. sensor for the simultaneous determination of xanthine (XA) and hypoxanthine (HX) based on poly(4-amino-3-hydroxy naphthalene-1-sulfonic acid) [p(AHNSA)] modified glassy carbon electrode (GCE) is reported here. The proposed sensor permit well resolved and well separated peaks for XA and HX in 0.1 M NaOH at comparably lowest potential by square wave voltammetric (SWV) technique. The exptl. parameters required for the electroxidn. of both XA and HX are optimized. For simultaneous determination, the oxidation peak current showed a linear variation in the concentration range 4.0 x 10-4-3.0 x 10-6 M and 2.0 x 10-4-6.0 x 10-6 M with detection limits 7.1 x 10-7 M and 1.5 x 10-6 M for XA for HX, resp. The mechanistic aspects were studied by linear sweep voltammetry (LSV) and the electrode processes were found to be diffusion controlled. The developed sensor was found to have promising application in some real samples like tea and coffee and in physiol. samples with good selectivity and sensitivity.

Journal of the Electrochemical Society published new progress about 116-63-2. 116-63-2 belongs to naphthyridine, auxiliary class Sulfonic acid,Amine,Naphthalene,Alcohol,Organic Pigment, name is 4-Amino-3-hydroxynaphthalene-1-sulfonic acid, and the molecular formula is C10H9NO4S, Application of 4-Amino-3-hydroxynaphthalene-1-sulfonic acid.

Referemce:
https://en.wikipedia.org/wiki/1,8-Naphthyridine,
1,8-Naphthyridine | C8H6N2 – PubChem

Jones, Suzanne F. published the artcileA phase I/II study of exisulind in combination with docetaxel/carboplatin in patients with metastatic non-small-cell lung cancer, Synthetic Route of 59973-80-7, the publication is Clinical Lung Cancer (2005), 6(6), 361-366, database is CAplus and MEDLINE.

Exisulind is a sulfone derivative of sulindac that induces apoptosis and demonstrates synergy with docetaxel in lung cancer models. This study evaluated the safety, efficacy, and pharmacokinetic interactions of exisulind and docetaxel/carboplatin in patients with metastatic non-small-cell lung cancer (NSCLC). Fifty-seven patients received 218 cycles of docetaxel (75 mg/m²) and carboplatin (area under the curve, 5.0) in combination with exisulind (125-250 mg orally twice daily). Two complete responses and 9 partial responses were observed among the 47 patients assessable for response (overall response rate, 23%). The median duration of response was 5.9 mo and median survival was 9.4 mo. The 1- and 2-yr survival rates are 35% and 14%, resp. The hematol. toxicities were consistent with those previously reported with docetaxel/carboplatin. The most common nonhematol. toxicities were mild to moderate fatigue, anorexia, nausea, and vomiting. The addition of exisulind to the chemotherapy regimen did not interfere with the metabolism or elimination of docetaxel and vice versa, and docetaxel did not interfere with the pharmacokinetic parameters of exisulind. This trial did not allow direct comparison of patients receiving docetaxel/carboplatin with and without exisulind, but when compared with historical data of docetaxel/carboplatin alone, the addition of exisulind does not appear to enhance antitumor activity, duration of response, or survival. Although preclin. data demonstrate increased apoptosis and prolonged survival for the combination of exisulind and docetaxel, multiple clin. trials do not support further clin. development of this combination regimen in patients with advanced NSCLC.

Clinical Lung Cancer published new progress about 59973-80-7. 59973-80-7 belongs to naphthyridine, auxiliary class Immunology/Inflammation,COX, name is Sulindac sulfone, and the molecular formula is C20H17FO4S, Synthetic Route of 59973-80-7.

Referemce:
https://en.wikipedia.org/wiki/1,8-Naphthyridine,
1,8-Naphthyridine | C8H6N2 – PubChem