Month: December 2022

Ashour, Abdelkader E. published the artcilePhosphodiesterase-5 inhibitors in the management of cancer, Synthetic Route of 59973-80-7, the publication is Asian Journal of Biomedical and Pharmaceutical Sciences (2013), 3(20), 1-5, 5 pp., database is CAplus.

A review. Selective phosphodiesterase type-5 (PDE5) inhibitors such as sildenafil, vardenafil and tadalafil are commonly used first-line therapy for erectile dysfunction (ED). The safety and high tolerability of these drugs has garnered substantial interest among researchers to investigate further beneficial nonerectogenic uses for such drugs. PDE5 expression has shown to be increased in several human malignancies, suggesting that this enzyme may play a role in tumorigenesis. This is supported by the reported anticancer activity of PDE5 inhibitors such as exisulinde and its analogs, as well as vardenafil. Further, PDE5 inhibitors have recently been reported to sensitize certain types of cancer to standard chemotherapeutic drugs. The aim of this review is to shed some light on the existing preclin. evidence supporting the use of PDE5 inhibitors as potential effective adjuncts in cancer chemotherapy and even as anticancer agents. I also showed our recent unpublished data with regard to the promising antitumor activity of vardenafil, a potent PDE5 inhibitor, against brain cancer.

Asian Journal of Biomedical and Pharmaceutical Sciences 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

Anonymous published the artcileExisulind. aptosyn, FGN 1, prevatac, sulindac sulfone, Formula: C20H17FO4S, the publication is Drugs in R&D (2004), 5(4), 220-226, database is CAplus.

A review. Exisulind [Aptosyn, FGN 1, Prevatac, sulindac sulfone], the sulfone derivative of sulindac, is the lead compound in a series of selective apoptotic antineoplastic drugs (SAANDs) being developed by OSI Pharmaceuticals. The compounds were originally developed by Cell Pathways, which was acquired by, and integrated into, OSI Pharmaceuticals in June 2003. Exisulind inhibits the enzyme cGMP phosphodiesterase (GMP-PDE), overexpressed in precancerous and cancerous colorectal cells, and induces apoptosis in such cells with minimal effects on normal cells. This apoptotic effect is independent of COX I or COX II inhibition, p53, Bcl-2, or cell-cycle arrest. Preclin. evidence suggests that exisulind also inhibits angiogenesis. Cell Pathways has formed sales and distribution agreements with three healthcare-related companies in the US for its future marketing and support campaign for exisulind. Innovex will hire and train sales representatives for Cell Pathways to launch and promote exisulind, Livingston Healthcare Services will be responsible for customer service, order and distribution administration, and Lash Group will be responsible for the development and implementation of reimbursement support services for exisulind. Cell Pathways has issued an exclusive license for exisulind to Paladin Labs of Montreal, Canada. The agreement allows Paladin exclusive rights to commercialise the drug in Canada. In August 1999 Cell Pathways submitted an NDA application to the US FDA for exisulind (Aptosyn) for the treatment of familial adenomatous polyposis (FAP). However, in Sept. 2000, the FDA announced that it had found deficiencies in the safety and efficacy data of Cell Pathways’ NDA, and returned a non-approvable letter to the company. Cell Pathways then initiated another phase III study of the agent in combination with Aventis’ docetaxel and comparing combination therapy with docetaxel alone. Exisulind has fast-track designation for FAP in the US. Phase I and II pediatric trials are also underway in the US. Cell Pathways announced in Apr. 2000 that it had completed enrollment in an open-label phase II study in children with familial adenomatous polyposis (FAP). Patients will be evaluated to determine whether polyp numbers have been reduced after 1 yr relative to baseline. In June 2000, Cell Pathways announced the results of a 1-yr extension of a 1997-1999 phase III trial that showed that exisulind significantly reduced polyp formation in patients with FAP. Enrollment of 282 patients in a multicentre, placebo-controlled phase III trial for the treatment of sporadic colonic polyps was completed in the US in May 1999. In its 2003 Annual Report, Paladin Labs announced that it is conducting a phase III study of exisulind in patients with prostate cancer in Canada. Exisulind has completed a pivotal phase II/III trial for preventing the recurrence of prostate cancer in the US. Two phase II prostate cancer trials were initiated in June 1999. The first study assessed the efficacy of exisulind in 15 patients who had undergone prostatectomy, were receiving LHRH-agonist hormone therapy and had increasing PSA levels (study EX1001). The second trial was to enrol 20 hormone-refractory patients scheduled for radical prostatectomy within 2-8 wk of diagnosis (study EX1004). This study compared the effect of exisulind + docetaxel on the rate of apoptosis and GMP-PDE expression in premalignant or malignant and normal prostate tissue. Cell Pathways and Rhone-Poulenc Rorer (now Aventis) agreed to collaborate on clin. trials of.exisulind in combination with docetaxel in the treatment of various solid tumors. The first phase I/II trial (study 026) was to enrol previously untreated patients with non-small cell lung cancer (NSCLC). OSI Pharmaceuticals and Bristol-Myers Squibb are conducting a phase I/II trial (study EX 2002) of exisulind in combination with paclitaxel and carboplatin as first-line treatment for patients with NSCLC. Both companies will share costs and information gathered from the trial. A phase I/II trial (study EX 2006) of weekly paclitaxel and carboplatin combined with exisulind is also underway in patients with advanced NSCLC. Cell Pathways and Glaxo Wellcome are cooperating in supporting a clin. trial (study EX 2004) of exisulind in combination with vinorelbine as first-line treatment for elderly patients with advanced NSCLC. The study will be conducted at the University of Wisconsin, and the two companies will share the costs of the trial while maintaining the rights to their resp. compounds Cell Pathways and Eli Lilly have a phase I/II trial (study EX 2005) of exisulind in- combination with gemcitabine underway in patients with NSCLC. This study will investigate the efficacy and tolerability of escalating doses of exisulind in combination with a standard gemcitabine regimen. The Cancer and Leukemia Group B (CALGB) initiated a phase 11 study of exisulind in combination with etoposide and carboplatin in patients with small cell lung cancer in the US in Sept. 2002. The Eastern Cooperative Oncol. Group (ECOG) initiated a phase 11 study in NSCLC patients in Sept. 2002 that will investigate the effects of exisulind in combination with gemcitabine and carboplatin. The objectives of the two studies are to determine the 12-mo survival rate and response rates following treatment with the combination regimens. Patents covering the mechanism of action of exisulind have been allowed in Europe and Japan, and extend to the methods of identifying compounds that selectively stimulate apoptosis in precancerous and cancerous cell.

Drugs in R&D 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, Formula: C20H17FO4S.

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

Xu, Bo published the artcile4-Tert-butylpyridine Free Organic Hole Transporting Materials for Stable and Efficient Planar Perovskite Solar Cells, Application of Spiro[fluorene-9,9′-xanthene], the publication is Advanced Energy Materials (2017), 7(19), n/a, database is CAplus.

4-Tert-butylpyridine (tBP) is an important additive in triarylamine-based organic hole-transporting materials (HTMs) for improving the efficiency and steady-state performance of perovskite solar cells (PVSCs). However, the low b.p. of tBP (196°C) significantly affects the long-term stability and device performance of PVSCs. Herein, the design and synthesis of a series of covalently linked Spiro[fluorene-9,9′-xanthene] (SFX)-based organic HTMs and pyridine derivatives to realize efficient and stable planar PVSCs are reported. One of the tailored HTMs, N2,N2,N7,N7-tetrakis(4-methoxyphenyl)-3′,6′-bis(pyridin-4-ylmethoxy) spiro[fluorene-9,9′-xanthene]-2,7-diamine (XPP) with two para-position substituted pyridines that immobilized on the SFX core unit shows a high power conversion efficiency (PCE) of 17.2% in planar CH₃NH₃PbI₃-based PVSCs under 100 mW cm^-2 AM 1.5G solar illumination, which is much higher than the efficiency of 5.5% that using the well-known 2,2′,7,7′-tetrakis-(N,N-di-p-methoxy-phenyl-amine)9,9′-spirobifluorene (Spiro-OMeTAD) as HTM (without tBP) under the same condition. Most importantly, the pyridine-functionalized HTM-based PVSCs without tBP as additive show much better long-term stability than that of the state-of-the-art HTM Spiro-OMeTAD-based solar cells that containing tBP as additive. This is the first case that the tBP-free HTMs are demonstrated in PVSCs with high PCEs and good stability. It paves the way to develop highly efficient and stable tBP-free HTMs for PVSCs toward com. applications.

Advanced Energy Materials published new progress about 159-62-6. 159-62-6 belongs to naphthyridine, auxiliary class Other Aromatic Heterocyclic,Spiro, name is Spiro[fluorene-9,9′-xanthene], and the molecular formula is C5H5F3O2, Application of Spiro[fluorene-9,9′-xanthene].

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

Zhu, Junchen published the artcileA novel C₂ symmetric chiral stationary phase with N-[(4-Methylphenyl)sulfonyl]-L-leucine as chiral side chains, Computed Properties of 2960-93-2, the publication is Journal of Separation Science (2020), 43(12), 2338-2348, database is CAplus and MEDLINE.

In this study, a series of chiral stationary phases based on N-[(4-methylphenyl)sulfonyl]-L-leucine amide, whose enantiorecognition property has never been studied, were synthesized. Their enantioseparation abilities were chromatog. evaluated by 67 enantiomers. The chiral stationary phase derived from N-[(4-methylphenyl)sulfonyl]-L-leucine showed much better enantioselectivities than that based on N-(4-methylbenzoyl)-L-leucine amide. The construction of C₂ sym. chiral structure greatly improved the enantiorecognition performance of the stationary phase. The C₂ sym. chiral stationary phase exhibited superior enantioresolns. to other chiral stationary phases for most of the chiral analytes, especially for the chiral analytes with C₂ sym. structures. By comparing the enantioseparations of the enantiomers with similar structures, the importance of hydrogen bond interaction, π-π interaction, and steric hindrance on enantiorecognition was elucidated. The enantiorecognition mechanism of trans-N,N’-(1,2-diphenyl-1,2-ethanediyl)bis-acetamide, which had an excellent separation factor on the C₂ sym. chiral stationary phase, was investigated by ¹H-NMR spectroscopy and 2D ¹H-¹H nuclear overhauser enhancement spectroscopy.

Journal of Separation Science published new progress about 2960-93-2. 2960-93-2 belongs to naphthyridine, auxiliary class Naphthalene,Ether,Other MOF ligands,Organic ligands for MOF materials, name is 2,2′-Dimethoxy-1,1′-binaphthalene, and the molecular formula is C14H10N2O, Computed Properties of 2960-93-2.

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

Liu, Yang published the artcileSynthesis and self-assembly of triblock oligomers containing anthracene unit, SDS of cas: 18512-55-5, the publication is Gaodeng Xuexiao Huaxue Xuebao (2014), 35(5), 989-994, database is CAplus.

Rod-coil mols., consisting of a flexible and a rigid block, have a strong tendency to self-organize into a various supramol. nanostructures in the bulk state. Two coil-rod-coil triblock cruciform compds incorporating anthracene unit were synthesized through Sonogashira coupling reaction. Mol. structures of these compounds were characterized by ¹H NMR and MALDI-TOF mass spectroscopy. The self-assembling behaviors of these mols. were investigated by means of differential scanning calorimetry (DSC), thermal polarized optical microscopy (POM), small-angle and wide-angle X-ray scattering (SAXS and WAXS) at the bulk state. In liquid crystalline mesophase, the compounds connecting with tetra(ethylene oxide) as flexible chains self-assembles into oblique columnar phase and nematic phase, while the compound containing alkyl flexible chain self-assembles into lamellar structure (L) in the solid state, and has not shown liquid crystalline phase.

Gaodeng Xuexiao Huaxue Xuebao 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, SDS of cas: 18512-55-5.

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

Jin, Guangri published the artcileSynthesis, self-assembly and spectroscopic analysis of 9,10-bis((4-(2-(2-(2-methoxyethoxy)ethoxy)ethoxy)phenyl)ethynyl)anthracene, Formula: C18H10, the publication is Yingyong Huaxue (2015), 32(2), 177-182, database is CAplus.

Compound I [R = O(CH₂CH₂O)₃OMe] was synthesized by Sonogashira coupling. Its structure was characterized by ¹H NMR and MALDI-TOF mass spectroscopy. The self-assembling behavior of compound I [R = O(CH₂CH₂O)₃OMe] was investigated by means of differential scanning calorimetry (DSC), thermal polarized optical microscopy (POM), and small-angle X-ray scattering (SAXS) at the bulk state. Compound I [R = O(CH₂CH₂O)₃OMe] self-assembled into smectic A phase (SmA) in the solid state. Spectroscopic anal. suggested that compound 1 inherited the characteristic of high fluorescence quantum yield (Φ_f) of disubstituted anthracenes. The title compound I [R = O(CH₂CH₂O)₃OMe] is a kind of photoluminescence materials with good performance.

Yingyong Huaxue 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, Formula: C18H10.

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

Qiu, Liqin published the artcilePalladium-Catalyzed Suzuki-Miyaura Coupling Reactions of Boronic Acid Derivatives with Aryl Chlorides, Application In Synthesis of 2960-93-2, the publication is Asian Journal of Organic Chemistry (2016), 5(10), 1260-1268, database is CAplus.

A series of new biphenyl N,P-monophosphine ligands were developed via introduction of two methoxy groups to the biphenyl backbone. The ligands were found to be much more effective than their counterparts Buchwald ligands in the Suzuki-Miyaura coupling reactions of sterically hindered and electron-rich aryl chlorides with aryl boronic acids. A variety of tri-ortho-substituted or tetra-ortho-substituted biaryls or hetero-biaryls were conveniently prepared in up to 99% yield using 2′-(diphenylphosphanyl)-6,6′-dimethoxy-N,N-dimethyl-[1,1′-biphenyl]-2-amine-[Pd₂(dba)₃] as the catalyst.

Asian Journal of Organic Chemistry published new progress about 2960-93-2. 2960-93-2 belongs to naphthyridine, auxiliary class Naphthalene,Ether,Other MOF ligands,Organic ligands for MOF materials, name is 2,2′-Dimethoxy-1,1′-binaphthalene, and the molecular formula is C22H18O2, Application In Synthesis of 2960-93-2.

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

Fu, Wai Chung published the artcileA benzo[c]carbazolyl-based phosphine ligand for Pd-catalyzed tetra-ortho-substituted biaryl syntheses, Category: naphthyridine, the publication is Organic Chemistry Frontiers (2016), 3(2), 273-276, database is CAplus.

A new benzo[c]carbazolyl-based phosphine ligand I has been designed and synthesized. This newly developed ligand I efficiently facilitates the Pd-catalyzed syntheses of tetra-ortho-substituted biaryl compounds RR¹ [R = C₆F₅, 2,3-dimethoxynaphthalen-1-yl, dimethyl-1,2-oxazol-4-yl, etc.; R¹ = 2,6-(CH₃)₂C₆H₃, 2,6-(CH₃O)₂C₆H₃, 2,4,6-(CH₃)₃C₆H₂, 2,6-(CH₃)₂-4-H₃COC₆H₂, 2-methoxynaphthalen-1-yl] via Suzuki-Miyaura cross-coupling. With 1 mol% of the Pd(OAc)₂/I catalyst, sterically congested biaryls were afforded in good-to-excellent yields. In particular, the mild reaction conditions exhibited good compatibility of heterocycles and functional groups including esters and nitrile. The ligand I was structurally characterized by X-ray crystallog. anal.

Organic Chemistry Frontiers published new progress about 2960-93-2. 2960-93-2 belongs to naphthyridine, auxiliary class Naphthalene,Ether,Other MOF ligands,Organic ligands for MOF materials, name is 2,2′-Dimethoxy-1,1′-binaphthalene, and the molecular formula is C22H18O2, Category: naphthyridine.

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

Li, Xiao-Zhen published the artcileMetal ion adaptive self-assembly of photoactive lanthanide-based supramolecular hosts, Product Details of C22H18O2, the publication is Chemical Communications (Cambridge, United Kingdom) (2020), 56(32), 4416-4419, database is CAplus and MEDLINE.

A post-synthetic transmetalation self-assembly strategy was developed for the preparation of near IR (NIR) emitting Yb₈L₆ cubes, which could not be synthesized through direct metal-ligand assembly procedures. Metal-adaptive critical structural transformations from La₆L₃ triangular prism to Ln₈L₆ cubes were observed along the lanthanide series, the latter of which showed size-selective guest binding behavior toward poly-aromatic hydrocarbon (PAH) mols.

Chemical Communications (Cambridge, United Kingdom) published new progress about 2960-93-2. 2960-93-2 belongs to naphthyridine, auxiliary class Naphthalene,Ether,Other MOF ligands,Organic ligands for MOF materials, name is 2,2′-Dimethoxy-1,1′-binaphthalene, and the molecular formula is C22H18O2, Product Details of C22H18O2.

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

Zhu, Jikai published the artcileSynthesis and self-assembly of oligomers containing cruciform 9,10-bis(arylethynyl)anthracene unit: formation of supramolecular nanostructures based on rod-length-dependent organization, HPLC of Formula: 18512-55-5, the publication is Tetrahedron (2014), 70(6), 1230-1235, database is CAplus.

Conjugated rod-coil mols., incorporating flexible and rigid blocks, have a strong affinity to self-organize into various supramol. nanostructures in the bulk state.In this study, we report synthesized oligomers containing cruciform 9,10-bis(arylethynyl)anthracene units and characterized their self-assembly behavior. The mol. structures were characterized with ¹H, ¹³C NMR, and matrix-assisted laser desorption ionization time-of-flight (MALDI-TOF) mass spectroscopy. An investigation of the supramol. nanostructures of these mols. using differential scanning calorimetry, thermal polarized optical microscopy, and small-angle X-ray scattering revealed that the rod length of coil-rod-coil mols. with identical rod to coil volume ratios dramatically influences self-assembly behavior in the bulk state.

Tetrahedron 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 C15H14O3, HPLC of Formula: 18512-55-5.

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