Tag: M.W=100-150

Kapara, Anastasia published the artcileDetection of Estrogen Receptor Alpha and Assessment of Fulvestrant Activity in MCF-7 Tumor Spheroids Using Microfluidics and SERS, Quality Control of 19959-71-8, the publication is Analytical Chemistry (Washington, DC, United States) (2021), 93(14), 5862-5871, database is CAplus and MEDLINE.

Breast cancer is one of the leading causes of cancer death in women. Novel in vitro tools that integrate three-dimensional (3D) tumor models with highly sensitive chem. reporters can provide useful information to aid biol. characterization of cancer phenotype and understanding of drug activity. The combination of surface-enhanced Raman scattering (SERS) techniques with microfluidic technologies offers new opportunities for highly selective, specific, and multiplexed nanoparticle-based assays. Here, we explored the use of functionalized nanoparticles for the detection of estrogen receptor alpha (ERα) expression in a 3D tumor model, using the ERα-pos. human breast cancer cell line MCF-7. This approach was used to compare targeted vs. nontargeted nanoparticle interactions with the tumor model to better understand whether targeted nanotags are required to efficiently target ERα. Mixtures of targeted anti-ERα antibody-functionalized nanotags (ERα-AuNPs) and nontargeted (against ERα) anti-human epidermal growth factor receptor 2 (HER2) antibody-functionalized nanotags (HER2-AuNPs), with different Raman reporters with a similar SERS signal intensity, were incubated with MCF-7 spheroids in microfluidic devices and spectroscopically analyzed using SERS. MCF-7 cells expressed high levels of ERα and no detectable levels of HER2. 2D and 3D SERS measurements confirmed the strong targeting effect of ERα-AuNP nanotags to the MCF-7 spheroids in contrast to HER2-AuNPs (63% signal reduction). Moreover, 3D SERS measurements confirmed the differentiation between the targeted and the nontargeted nanotags. Finally, we demonstrated how the nanotag uptake on MCF-7 spheroids was affected by the drug fulvestrant, the first-in-class approved selective estrogen receptor degrader (SERD). These results illustrate the potential of using SERS and microfluidics as a powerful in vitro platform for the characterization of 3D tumor models and the investigation of SERD activity.

Analytical Chemistry (Washington, DC, United States) published new progress about 19959-71-8. 19959-71-8 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Pyridine, name is 4-(1H-Pyrazol-4-yl)pyridine, and the molecular formula is C8H7N3, Quality Control of 19959-71-8.

Referemce:
https://en.wikipedia.org/wiki/Pyrazole,
Pyrazoles – an overview | ScienceDirect Topics

Buckley, George M. published the artcileIRAK-4 inhibitors. Part III: A series of imidazo[1,2-a]pyridines, Computed Properties of 724710-02-5, the publication is Bioorganic & Medicinal Chemistry Letters (2008), 18(12), 3656-3660, database is CAplus and MEDLINE.

Following the identification of a potent IRAK inhibitor through routine project cross screening, a novel class of IRAK-4 inhibitor was established. The SAR of imidazo[1,2-a]pyridino-pyridines and benzimidazolo-pyridines was explored.

Bioorganic & Medicinal Chemistry Letters published new progress about 724710-02-5. 724710-02-5 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Boronic acid and ester,Pyrazole,Boronic Acids,Boronic acid and ester, name is (1H-Pyrazol-5-yl)boronic acid, and the molecular formula is C3H5BN2O2, Computed Properties of 724710-02-5.

Referemce:
https://en.wikipedia.org/wiki/Pyrazole,
Pyrazoles – an overview | ScienceDirect Topics

Fritzemeier, Russell published the artcileDiscovery of In Vivo Active Sphingosine-1-phosphate Transporter (Spns2) Inhibitors, Synthetic Route of 724710-02-5, the publication is Journal of Medicinal Chemistry (2022), 65(11), 7656-7681, database is CAplus and MEDLINE.

Sphingosine 1-phosphate (S1P) is a pleiotropic signaling mol. that interacts with five G-protein-coupled receptors (S1P1-5) to regulate cellular signaling pathways. S1P export is facilitated by Mfsd2b and spinster homolog 2 (Spns2). While mouse genetic studies suggest that Spns2 functions to maintain lymph S1P, Spns2 inhibitors are necessary to understand its biol. and to learn whether Spns2 is a viable drug target. Herein, we report a structure-activity relationship study that identified the first Spns2 inhibitor 16d (SLF1081851)(I). In vitro studies in HeLa cells demonstrated that 16d inhibited S1P release with an IC₅₀ of 1.93 μM. Administration of 16d to mice and rats drove significant decreases in circulating lymphocyte counts and plasma S1P concentrations, recapitulating the phenotype observed in mice made deficient in Spns2. Thus, 16d has the potential for development and use as a probe to investigate Spns2 biol. and to determine the potential of Spns2 as a drug target.

Journal of Medicinal Chemistry published new progress about 724710-02-5. 724710-02-5 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Boronic acid and ester,Pyrazole,Boronic Acids,Boronic acid and ester, name is (1H-Pyrazol-5-yl)boronic acid, and the molecular formula is C3H5BN2O2, Synthetic Route of 724710-02-5.

Referemce:
https://en.wikipedia.org/wiki/Pyrazole,
Pyrazoles – an overview | ScienceDirect Topics

Fritzemeier, Russell published the artcileDiscovery of In Vivo Active Sphingosine-1-phosphate Transporter (Spns2) Inhibitors, Related Products of pyrazoles-derivatives, the publication is Journal of Medicinal Chemistry (2022), 65(11), 7656-7681, database is CAplus and MEDLINE.

Sphingosine 1-phosphate (S1P) is a pleiotropic signaling mol. that interacts with five G-protein-coupled receptors (S1P1-5) to regulate cellular signaling pathways. S1P export is facilitated by Mfsd2b and spinster homolog 2 (Spns2). While mouse genetic studies suggest that Spns2 functions to maintain lymph S1P, Spns2 inhibitors are necessary to understand its biol. and to learn whether Spns2 is a viable drug target. Herein, we report a structure-activity relationship study that identified the first Spns2 inhibitor 16d (SLF1081851)(I). In vitro studies in HeLa cells demonstrated that 16d inhibited S1P release with an IC₅₀ of 1.93 μM. Administration of 16d to mice and rats drove significant decreases in circulating lymphocyte counts and plasma S1P concentrations, recapitulating the phenotype observed in mice made deficient in Spns2. Thus, 16d has the potential for development and use as a probe to investigate Spns2 biol. and to determine the potential of Spns2 as a drug target.

Journal of Medicinal Chemistry published new progress about 763120-58-7. 763120-58-7 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Boronic acid and ester,Boronic Acids,Boronic acid and ester, name is 1H-Pyrazole-4-boronic acid, and the molecular formula is C3H5BN2O2, Related Products of pyrazoles-derivatives.

Referemce:
https://en.wikipedia.org/wiki/Pyrazole,
Pyrazoles – an overview | ScienceDirect Topics

Engers, Darren W. published the artcileSynthesis and structure-activity relationships of a novel and selective bone morphogenetic protein receptor (BMP) inhibitor derived from the pyrazolo[1.5-a]pyrimidine scaffold of Dorsomorphin: The discovery of ML347 as an ALK2 versus ALK3 selective MLPCN probe, Recommanded Product: 1H-Pyrazole-4-boronic acid, the publication is Bioorganic & Medicinal Chemistry Letters (2013), 23(11), 3248-3252, database is CAplus and MEDLINE.

A structure-activity relation of the 3- and 6-positions of the pyrazolo[1,5-a]pyrimidine scaffold of the known BMP inhibitors dorsomorphin, 1, LDN-193189, 2, and DMH1, 3, led to the identification of a potent and selective compound for ALK2 vs. ALK3. The potency contributions of several 3-position substituents were evaluated with subtle structural changes leading to significant changes in potency. From these studies, a novel 5-quinoline mol. was identified and designated an MLPCN probe mol., ML347, which shows >300-fold selectivity for ALK2 and presents the community with a selective mol. probe for further biol. evaluation.

Bioorganic & Medicinal Chemistry Letters published new progress about 763120-58-7. 763120-58-7 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Boronic acid and ester,Boronic Acids,Boronic acid and ester, name is 1H-Pyrazole-4-boronic acid, and the molecular formula is C3H5BN2O2, Recommanded Product: 1H-Pyrazole-4-boronic acid.

Referemce:
https://en.wikipedia.org/wiki/Pyrazole,
Pyrazoles – an overview | ScienceDirect Topics

Tironi, Carla published the artcilePyrazole sulfanilamides: nitro derivatives of 1-phenyl-3-sulfanilamidopyrazole, Recommanded Product: 3-Acetamidopyrazole, the publication is Farmaco (1990), 45(4), 473-8, database is CAplus and MEDLINE.

The synthesis and structural characterization of 3 title compounds I (R = 2-O₂N, 3-O₂N, 4-O₂N) from 3(5)-acetamidopyrazole and RC₆H₄Br are reported. All derivatives are analyzed by ¹H and ¹³C NMR spectroscopy. The min. inhibiting concentration values obtained against Escherichia coli are briefly discussed in terms of structure-activity relationship.

Farmaco published new progress about 3553-12-6. 3553-12-6 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Amine,Amide, name is 3-Acetamidopyrazole, and the molecular formula is C10H11FN2O2S, Recommanded Product: 3-Acetamidopyrazole.

Referemce:
https://en.wikipedia.org/wiki/Pyrazole,
Pyrazoles – an overview | ScienceDirect Topics

Nasveschuk, Christopher G. published the artcileDiscovery and Optimization of Tetramethylpiperidinyl Benzamides as Inhibitors of EZH2, Name: 1H-Pyrazole-4-boronic acid, the publication is ACS Medicinal Chemistry Letters (2014), 5(4), 378-383, database is CAplus and MEDLINE.

The identification and development of a novel series of small mol. Enhancer of Zeste Homolog 2 (EZH2) inhibitors is described. A concise and modular synthesis enabled the rapid development of structure-activity relationships, which led to the identification of I as a potent, SAM-competitive inhibitor of EZH2 that dose-dependently decreased global H3K27me3 in KARPAS-422 lymphoma cells.

ACS Medicinal Chemistry Letters published new progress about 763120-58-7. 763120-58-7 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Boronic acid and ester,Boronic Acids,Boronic acid and ester, name is 1H-Pyrazole-4-boronic acid, and the molecular formula is C3H5BN2O2, Name: 1H-Pyrazole-4-boronic acid.

Referemce:
https://en.wikipedia.org/wiki/Pyrazole,
Pyrazoles – an overview | ScienceDirect Topics

Brzozowski, Zdzislaw published the artcileDerivatives of pyrazole-1-carboxylic acid. V. Syntheses of some derivatives of N-{4-[2-(pyrazole-1-carboxamido)ethyl]benzensulfonyl}-2-pyrazoline-1-carboxamide, Category: pyrazoles-derivatives, the publication is Acta Poloniae Pharmaceutica (1982), 39(1-3), 15-19, database is CAplus.

Twenty-five title compounds I (R-R⁶ = H, Me, and Et in various combinations) were prepared in 17-73% yields in the reaction of II with appropriately substituted pyrazole-1-carboxylic acid chlorides in the presence of 40% aqueous NaOH. Nine of them showed a moderate hypoglycemic activity in exptl. rats.

Acta Poloniae Pharmaceutica published new progress about 53355-55-8. 53355-55-8 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Chloride,acyl chloride,Amide, name is 1H-Pyrazole-1-carbonyl chloride, and the molecular formula is C4H3ClN2O, Category: pyrazoles-derivatives.

Referemce:
https://en.wikipedia.org/wiki/Pyrazole,
Pyrazoles – an overview | ScienceDirect Topics

Shan, Yuanyuan published the artcileDiscovery of novel VEGFR-2 inhibitors. Exploration of diverse hinge-binding fragments via core-refining approach, Recommanded Product: 1H-Pyrazole-4-boronic acid, the publication is European Journal of Medicinal Chemistry (2015), 80-90, database is CAplus and MEDLINE.

Pathol. angiogenesis plays a critical role in numerous diseases including malignancy. VEGFR-2 is the central regulators in angiogenesis and has become a promising target for anticancer drug design. The authors have identified a novel biphenyl-aryl urea incorporated with salicyladoxime (BPS-7) as potent VEGFR-2 inhibitor. As a continuation to the previous research, various aromatic-heterocyclic were introduced as hinge-binding fragment via a core-refining approach. Interestingly, many compounds exhibited comparable VEGFR-2 inhibition to Sorafenib. In particular, I and II displayed excellent VEGFR-2 inhibitory activity with IC₅₀ values of 0.50 nM and 0.79 nM, resp. Several title compounds showed considerable antiproliferative activity against A549 and SMMC-7721 cells. In addition, mol. docking was performed to rationalize the efficiency of the better compounds These results will be instructive for further inhibitor design and optimization.

European Journal of Medicinal Chemistry published new progress about 763120-58-7. 763120-58-7 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Boronic acid and ester,Boronic Acids,Boronic acid and ester, name is 1H-Pyrazole-4-boronic acid, and the molecular formula is C27H39ClN2, Recommanded Product: 1H-Pyrazole-4-boronic acid.

Referemce:
https://en.wikipedia.org/wiki/Pyrazole,
Pyrazoles – an overview | ScienceDirect Topics