Month: December 2022

Zhu, Yongyan published the artcileVinblastine-Loaded Nanoparticles with Enhanced Tumor-Targeting Efficiency and Decreasing Toxicity: Developed by One-Step Molecular Imprinting Process, Name: H-Lys(Boc)-OH, the publication is Molecular Pharmaceutics (2019), 16(6), 2675-2689, database is CAplus and MEDLINE.

Molecularly imprinted polymers have exhibited good performance as carriers on drug loading and sustained release. In this paper, vinblastine (VBL)-loaded polymeric nanoparticles (VBL-NPs) were prepared by a one-step mol. imprinting process, avoiding the waste and incomplete removal of the template, and evaluated as targeting carriers for VBL delivery after modification. Using acryloyl amino acid comonomers and disulfide cross-linkers, VBL-NPs were synthesized and then conjugated with poly(ethylene glycol)-folate. The dynamic size of the obtained VBL-NPs-PEG-FA was 258.3 nm (PDI = 0.250), and the encapsulation efficiency was 45.82 ± 1.45%. The nanoparticles of VBL-NPs-PEG-FA were able to completely release VBL during 48 h under a mimic tumor intracellular condition (pH 4.5, 10 mM glutathione (GSH)), displaying significant redox responsiveness, whereas the release rates were much slower in the mimic body liquid (pH 7.4, 2μM GSH) and tumor extracellular environment (pH 6.5, 2μM GSH). Furthermore, the carriers NPs-PEG-FA, prepared without VBL, showed satisfactory intrinsic hemocompatibility, cellular compatibility, and tumor-targeting properties: they could rapidly and efficiently accumulate to folate receptor pos. Hela cells and then internalized via receptor-mediated endocytosis, and the retention in tumor tissues could last for over 48 h. Interestingly, VBL-NPs-PEG-FA could evidently increase the accumulation of VBL in tumor tissues while decreasing the distribution of VBL in organs, exert similar anticancer efficacy against Hela tumors in the xenograft model of nude mice to VBL injection, and significantly improve the abnormality of liver and spleen observed in VBL injection. VBL-NPs-PEG-FA has the potential to be the delivery carrier for VBL by enhancing the tumor-targeting efficacy of VBL and decreasing toxicity to normal tissues.

Molecular Pharmaceutics published new progress about 2418-95-3. 2418-95-3 belongs to amides-buliding-blocks, auxiliary class Chiral,Carboxylic acid,Amine,Aliphatic hydrocarbon chain,Ester,Amino acide derivatives, name is H-Lys(Boc)-OH, and the molecular formula is C13H15NO6S, Name: H-Lys(Boc)-OH.

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

Marshall, Glenn M. published the artcileSIRT1 promotes N-Myc oncogenesis through a positive feedback loop involving the effects of MKP3 and ERK on N-Myc protein stability, Safety of 4-(tert-Butyl)-N-((4-(5-(dimethylamino)pentanamido)phenyl)carbamothioyl)benzamide, the publication is PLoS Genetics (2011), 7(6), e1002135, database is CAplus and MEDLINE.

The N-Myc oncoprotein is a critical factor in neuroblastoma tumorigenesis which requires addnl. mechanisms converting a low-level to a high-level N-Myc expression. N-Myc protein is stabilized when phosphorylated at Serine 62 by phosphorylated ERK protein. Here we describe a novel pos. feedback loop whereby N-Myc directly induced the transcription of the class III histone deacetylase SIRT1, which in turn increased N-Myc protein stability. SIRT1 binds to Myc Box I domain of N-Myc protein to form a novel transcriptional repressor complex at gene promoter of mitogen-activated protein kinase phosphatase 3 (MKP3), leading to transcriptional repression of MKP3, ERK protein phosphorylation, N-Myc protein phosphorylation at Serine 62, and N-Myc protein stabilization. Importantly, SIRT1 was up-regulated, MKP3 down-regulated, in pre-cancerous cells, and preventative treatment with the SIRT1 inhibitor Cambinol reduced tumorigenesis in TH-MYCN transgenic mice. Our data demonstrate the important roles of SIRT1 in N-Myc oncogenesis and SIRT1 inhibitors in the prevention and therapy of N-Myc-induced neuroblastoma.

PLoS Genetics published new progress about 1011557-82-6. 1011557-82-6 belongs to amides-buliding-blocks, auxiliary class Epigenetics,Sirtuin, name is 4-(tert-Butyl)-N-((4-(5-(dimethylamino)pentanamido)phenyl)carbamothioyl)benzamide, and the molecular formula is C25H34N4O2S, Safety of 4-(tert-Butyl)-N-((4-(5-(dimethylamino)pentanamido)phenyl)carbamothioyl)benzamide.

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

Robichaud, Brian A. published the artcileTitanium isopropoxide/pyridine mediated Knoevenagel reactions, SDS of cas: 15029-36-4, the publication is Tetrahedron Letters (2011), 52(51), 6935-6938, database is CAplus.

A Ti(OiPr)₄-pyridine-mediated Knoevenagel reaction between aromatic ketones and cyanoacetamides to provide Knoevenagel olefin products in good to excellent yields was reported. Almost in all cases studied, a single geometrical isomer was formed and isolated under the Ti(OiPr)₄-pyridine condensation conditions. This methodol. was also demonstrated as highly effective process between some other Knoevenagel active methylene compounds and aromatic ketones.

Tetrahedron Letters published new progress about 15029-36-4. 15029-36-4 belongs to amides-buliding-blocks, auxiliary class Nitrile,Amine,Aliphatic hydrocarbon chain,Amide, name is 2-Cyano-N-ethylacetamide, and the molecular formula is C5H8N2O, SDS of cas: 15029-36-4.

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

Dong, Peng published the artcileThe enhanced antitumor activity of the polymeric conjugate covalently coupled with docetaxel and docosahexaenoic acid, Formula: C11H22N2O4, the publication is Biomaterials Science (2022), 10(13), 3454-3465, database is CAplus and MEDLINE.

Docetaxel (DTX) has been widely used for the treatment of many types of cancer. However, DTX is poorly water-soluble and com. DTX is formulated in non-ionic surfactant polysorbate 80 and ethanol, thereby leading to hypersensitivity and serious side effects. Herein, a polymer dual drug conjugate was synthesized by coupling DTX and docosahexaenoic acid (DHA) with bifunctionalized dextran. The polysaccharide conjugate dextran-DHA-DTX possessed high water solubility and was self-assembled into nanoparticles with a diameter of 98.0 ± 6.4 nm. Pharmacokinetic and biodistribution studies showed that the dextran-DHA-DTX dual drug conjugate not only had significantly prolonged blood circulation but was also selectively accumulated in the tumor with reduced drug distribution in normal tissues. The conjugate exhibited a superior therapeutic effect in both xenograft nude mice models without causing any systemic side effects. Notably, the conjugate nearly eliminated all xenograft tumors in nude mice bearing breast cancer cells MCF-7. This study revealed that the dextran-based dual drug delivery system may provide an effective strategy to selectively deliver DTX to tumor sites.

Biomaterials Science published new progress about 2418-95-3. 2418-95-3 belongs to amides-buliding-blocks, auxiliary class Chiral,Carboxylic acid,Amine,Aliphatic hydrocarbon chain,Ester,Amino acide derivatives, name is H-Lys(Boc)-OH, and the molecular formula is C11H22N2O4, Formula: C11H22N2O4.

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

Wang, Feng published the artcileHighly efficient iron(II) chloride/N-bromosuccinimide-mediated synthesis of imides and acylsulfonamides, Recommanded Product: 2,4-Dichlorobenzamide, the publication is Advanced Synthesis & Catalysis (2009), 351(1+2), 246-252, database is CAplus.

The authors have developed a simple, general and highly efficient method for the synthesis of imides R¹C(O)NHC(O)R² (R¹ = Ph, 4-MeOC₆H₄, 4-BrC₆H₄; R² = Et, Pr, Ph, etc.) and acylsulfonamides, e.g. R³S(O)₂NHC(O)R⁴ (R³ = Ph, 4-MeC₆H₄, 4-ClC₆H₄, etc.; Et, Pr, Ph, etc.), via couplings of thioesters R⁵SC(O)R² (R⁵ = Me, Et) and R⁶SC(O)R⁴ (R⁶ = Me, Et) with carboxamides R¹C(O)NH₃ or sulfonamides R³S(O)₂NH₂ mediated by iron(II) chloride in the presence of N-bromosuccinimide.

Advanced Synthesis & Catalysis published new progress about 2447-79-2. 2447-79-2 belongs to amides-buliding-blocks, auxiliary class Chloride,Amine,Benzene,Amide, name is 2,4-Dichlorobenzamide, and the molecular formula is C65H82N2O18S2, Recommanded Product: 2,4-Dichlorobenzamide.

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

Zhou, Jianlin published the artcileSelf-Healing Titanium Dioxide Nanocapsules-Graphene/Multi-Branched Polyurethane Hybrid Flexible Film with Multifunctional Properties toward Wearable Electronics, Application In Synthesis of 2479-62-1, the publication is Advanced Functional Materials (2021), 31(29), 2011133, database is CAplus.

The integration of self-healing capabilities into flexible electronics arouses extensive attention. The application of self-healing electronics with multifunctional properties in a variety of exceptional environments has been identified to be significantly challenging and not yet proven to be fully viable thus far. In the present study, the self-healing octadecane loaded titanium dioxide nanocapsules (OTNs)-graphene/multi-branched polyurethane (PU) hybrid flexible multifunctional film is successfully prepared The prepared film exhibits a novel self-repair capability that consists of disulfide bonds in the leading chains for efficient self-healing of PU damage, as well as multiple amino groups in the branches for damage between OTNs-graphene and PU. Impacted by the constructed self-healing system and well-dispersed OTNs-graphene, the prepared flexible film demonstrates a prominent performance in piezoresistive sensing and a desirable outcome of UV protection properties, which can effectively prolong its service life, especially when used outdoors. Moreover, the film exhibits thermal insulating properties, capable of offering a suitable route for thermal protection of bio-integrated wearable electronic devices system. Thus, this self-healing multifunctional film is promising in wearable electronics, human-machine interaction, artificial intelligence devices, etc.

Advanced Functional Materials published new progress about 2479-62-1. 2479-62-1 belongs to amides-buliding-blocks, auxiliary class Monomers,Acrylamide Monomers, name is N-(2-Amino-2-oxoethyl)acrylamide, and the molecular formula is C15H24S, Application In Synthesis of 2479-62-1.

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

Zhou, Jianlin published the artcileDual Self-Healing Anticorrosion Coatings Based on Multibranched Waterborne Polyurethane and TiO₂ Nanocapsule-Loaded Graphene Oxide, Quality Control of 2479-62-1, the publication is Advanced Materials Interfaces (2022), 9(9), 2102001, database is CAplus.

The study reports the successful fabrication of a novel dual self-healing anticorrosion coating based on benzotriazole loaded TiO₂ nanocapsule (BTC) modified graphene oxide sheets and the multibranched waterborne polyurethane (WPU). When corrosion occurs, the benzotriazole (BZT) in nanocapsules can be slowly released from the coating forming a passivation layer on the metal surface to isolate the corrosive mediums. The anticorrosion performance of coating is examined by performing electrochem. tests. As indicated from the results, after being immersed in 3.5 wt% NaCl for 7 d, the prepared coating shows excellent anticorrosion performance with inhibition efficiency of 99%. In addition, the φ in 10⁴ Hz increases from 10° to 30°, and Log|Z|_0.01Hz remains at nearly 4.5 with the immersing time extended to 30 d. Moreover, when the coating is phys. damaged, the damaged coating can be self-repaired by the reversible disulfide bonds in WPU and the releasing of the BZT simultaneously. Compared with other control anticorrosion coatings, the healed coating achieves significantly improved anticorrosion performance, and the damaged coating can still sustain the original anticorrosion performance after self-healing. This study proposes a novel fabrication strategy for self-healing materials, and it can contribute to the long-term use of anticorrosion coatings.

Advanced Materials Interfaces published new progress about 2479-62-1. 2479-62-1 belongs to amides-buliding-blocks, auxiliary class Monomers,Acrylamide Monomers, name is N-(2-Amino-2-oxoethyl)acrylamide, and the molecular formula is C8H16O2, Quality Control of 2479-62-1.

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

Heemstra, Jennifer M. published the artcileTemplated Synthesis of Peptide Nucleic Acids via Sequence-Selective Base-Filling Reactions, Name: 2-(N-(2-((((9H-Fluoren-9-yl)methoxy)carbonyl)amino)ethyl)-2-(2-(((benzhydryloxy)carbonyl)amino)-6-oxo-5H-purin-9(6H)-yl)acetamido)acetic acid, the publication is Journal of the American Chemical Society (2009), 131(32), 11347-11349, database is CAplus and MEDLINE.

The templated synthesis of nucleic acids has previously been achieved through the backbone ligation of preformed nucleotide monomers or oligomers. In contrast, the authors, here, demonstrate templated nucleic acid synthesis using a base-filling approach in which individual bases are added to abasic sites of a peptide nucleic acid (PNA). Because nucleobase substrates in this approach are not self-reactive, a base-filling approach may reduce the formation of non-templated reaction products. Using either reductive amination or amine acylation chemistries, the authors observed efficient and selective addition of each of the four nucleobases to an abasic site in the middle of the PNA strand. The authors also describe the addition of single nucleobases to the end of a PNA strand through base filling, as well as the tandem addition of two bases to the middle of the PNA strand. These findings represent an exptl. foundation for nonenzymic information transfer through base filling.

Journal of the American Chemical Society published new progress about 186046-83-3. 186046-83-3 belongs to amides-buliding-blocks, auxiliary class Purine,Carboxylic acid,Amine,Benzene,Amide,Others,PNA,, name is 2-(N-(2-((((9H-Fluoren-9-yl)methoxy)carbonyl)amino)ethyl)-2-(2-(((benzhydryloxy)carbonyl)amino)-6-oxo-5H-purin-9(6H)-yl)acetamido)acetic acid, and the molecular formula is C40H35N7O8, Name: 2-(N-(2-((((9H-Fluoren-9-yl)methoxy)carbonyl)amino)ethyl)-2-(2-(((benzhydryloxy)carbonyl)amino)-6-oxo-5H-purin-9(6H)-yl)acetamido)acetic acid.

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

Duan, Wenlong published the artcilePolymorphs and Transformations of the Solid Forms of Organic Salts of 5-Sulfosalicylic Acid and Isonicotinamide, Recommanded Product: Isonicotinamide, the publication is Crystal Growth & Design (2020), 20(12), 7606-7614, database is CAplus.

Diversities of salts formed by 5-sulfosalicylic acid (5-SSA) and isonicotinamide (INA) were obtained by mechanochem. grinding and from solution, including 3 polymorphs of (5-SSA-2H)^–·(INA-H)⁺·H₂O (1) (form 1a, form 1b, and form 1c), dehydration phase (5-SSA-2H)₂^–·(INA-H)₂⁺ (2), solvent phases (5-SSA-2H)^–·(INA-H)⁺·MeOH (3) and (5-SSA-2H)₂^–·(INA-H)₂⁺·H₂O·MeOH (4), and stoichiometric form (5-SSA-2H)^–·(INA-H)⁺·(INA) (5). The work studies not only the stabilities of the 3 polymorphs and the relation between solvated 1 and desolvation phase 2 but also the interconversion of these crystalline phases. The dehydrated phase 2 and solvent phase 4 comprising 2 independent 5-SSA anions and 2 independent INA cations in the asym. unit form an individual ion pair and the corresponding H bonded networks. The solvent phase (5-SSA-2H)₂^–·(INA-H)₂⁺·H₂O·MeOH (4) shows the individual structural features of both (5-SSA-2H)^–·(INA-H)⁺·H₂O (1) and solvent phase (5-SSA-2H)^–·(INA-H)⁺·MeOH (3). All 7 salts build up layered structures but comprising a different H bonding network and can experience a reversible transformation. Quantum mechanics calculations are used to assess the stability of some of the crystalline phases under study. The example of salts of 5-SSA and INA comprising a diversity of solid forms reported here can be considered very rare, which provided a good model for the insight into the structural transformation of materials of interest. Diversities of salts formed by 5-sulfosalicylic acid (5-SSA) and isonicotinamide (INA), including 3 polymorphs of (5-SSA-2H)^–·(INA-H)⁺·H₂O (1), dehydrated (5-SSA-2H)₂^–·(INA-H)₂⁺ (2), solvent phases (5-SSA-2H)^–·(INA-H)⁺·MeOH (3) and (5-SSA-2H)₂^–·(INA-H)₂⁺·H₂O·MeOH (4), and stoichiometric form (5-SSA-2H)^–·(INA-H)⁺·(INA) (5), were obtained, and their reversible transformations were discussed.

Crystal Growth & Design published new progress about 1453-82-3. 1453-82-3 belongs to amides-buliding-blocks, auxiliary class Pyridine,Amine,Amide, name is Isonicotinamide, and the molecular formula is C6H6N2O, Recommanded Product: Isonicotinamide.

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

Yan, Zhongzhong published the artcileDesign, synthesis, DFT study and antifungal activity of the derivatives of pyrazolecarboxamide containing thiazole or oxazole ring, Recommanded Product: 2,4-Dichlorobenzamide, the publication is European Journal of Medicinal Chemistry (2018), 170-181, database is CAplus and MEDLINE.

To discover new pyrazolecarboxamide analogs with broad spectrum and high activity, a class of new compounds of pyrazole carboxamide derivatives containing thiazole or oxazole ring I (R¹ = H, 4-Me, 2-Cl, etc.; R² = H, Cl, Me; R³ = Me, Et, i-Pr, cyclopropyl; R⁴ = H, Et, Me, Ph; Z = S, O) was designed by scaffold hopping and bioisosterism, and 36 pyrazole carboxamide derivatives with antifungal activity were synthesized. Those compounds I were evaluated against five phytopathogenic fungi, Gibberella zeae, Phytophythora capsici, Sclerotonia sclerotiorum, Erysiphe graminis and Puccinia sorghi. The results indicated that most of the compounds displayed good fungicidal activities, especially against E. graminis. Theor. calculations were carried out at the B3LYP/6-31G (d, p) level and the full geometry optimization was carried out using the 6-31G (d, p) basis set, and the frontier orbital energy, at. net charges and, mol. docking were discussed, and the structure-activity relationships were also studied.

European Journal of Medicinal Chemistry published new progress about 2447-79-2. 2447-79-2 belongs to amides-buliding-blocks, auxiliary class Chloride,Amine,Benzene,Amide, name is 2,4-Dichlorobenzamide, and the molecular formula is C14H19NO8, Recommanded Product: 2,4-Dichlorobenzamide.

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