Month: December 2022

Bulat, Elif published the artcileNi(II) complexes with 1,3,2,4-dithiadiphosphetane 2,4-disulfide-based ligands: Structural insights, theoretical studies, and anticancer activities, COA of Formula: C5H12O, the main research area is nickel dimethoxyphenyl dithiadiphosphetane disulfide complex preparation crystal mol structure; anticancer activity mol structure calculation dithiadiphosphetane disulfide nickel complex.

The first synthesis of 2,4-bis(3,4-dimethoxyphenyl)-1,3-dithia-2,4-diphosphetane 2,4-disulfide (SAV-A1 reagent) was achieved. Seven oxo-alkyl esters (HLn) were synthesized thereof. Ni(II) complexes ([Ni(Ln)2]) of these ligands were prepared in ethanol. The structures were identified by spectral studies. Ni(II) complexes were unambiguously determined by x-ray crystallog. In addition, the ligands and their Ni(II) complexes were tested on two different human cancer cell lines, including liver and colon. Moreover, d. functional theory (DFT) calculations of the Ni(II) complexes were performed, and the mol. docking studies of these compounds with liver cancer protein, PDB ID: 3WZE and colon cancer antigen proteins, ID 2HQ6 were presented to investigate and predict potential interactions. P4S10.

Applied Organometallic Chemistry published new progress about Antitumor agents. 584-02-1 belongs to class alcohols-buliding-blocks, name is 3-Pentanol, and the molecular formula is C5H12O, COA of Formula: C5H12O.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Ji, Hai-yu published the artcileEffects of Heat Treatment on the Structural Characteristics and Antitumor Activity of Polysaccharides from Grifola frondosa, HPLC of Formula: 59-23-4, the main research area is Grifola polysaccharide antitumor agent heat treatment hepatocellular carcinoma; Antitumor; Heat treatment; Polysaccharides from Grifola frondosa; Structure.

This study investigated the effects of heat treatment on structural characteristics and in vitro antitumor activity of polysaccharides from Grifola frondosa. GFP-4 (extracted at 4°C), GFP-4-80 (80°C treatment on GFP-4) and GFP-80 (extracted at 80°C) were prepared, and the chem. composition anal. showed that their total sugar contents were all higher than 90%, high-performance gel-permeation chromatog. (HPGPC), ion chromatog. (IC) and Fourier-transform IR spectroscopy (FTIR) results demonstrated that GFP-4 were degraded and denatured after 80°C heat treatment, MTT and JC-1 results showed that GFP-4 exhibited higher inhibitory effects on HepG2 cells in vitro than GFP-4-80 and GFP-80. Our study suggested that heat treatment at 80°C on polysaccharides from Grifola frondosa would destroy their structure and attenuate their antitumor effects.

Applied Biochemistry and Biotechnology published new progress about Antitumor agents. 59-23-4 belongs to class alcohols-buliding-blocks, name is (2R,3S,4S,5R)-2,3,4,5,6-Pentahydroxyhexanal, and the molecular formula is C6H12O6, HPLC of Formula: 59-23-4.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Du, Baoxiang published the artcileIsolation, purification, structural analysis and biological activities of water-soluble polysaccharide from Glehniae radix, Name: (2R,3S,4S,5R)-2,3,4,5,6-Pentahydroxyhexanal, the main research area is Glehniae lung cancer polysaccharide antiinflammatory anticancer; Biological activities; Glehniae radix polysaccharide; Structural analysis.

A new polysaccharide named GRP (Glehniae radix polysaccharide) was isolated and purified from Glehniae radix by hot water extraction, ethanol precipitation, anion-exchange and gel-filtration chromatog. GRP was homogeneous, with a mol. weight of 1.33 × 104 Da, as determined by high-performance size-exclusion chromatog.-refractive index detector anal. Its structural characteristics were investigated and elucidated by methylation anal., gas chromatog. mass spectrometry, Fourier transform IR and NMR spectroscopy. Based on obtained data, GRP was found to be a-D-glucan containing (1-6)-linked and (1-3)-linked backbone with a branch of one (1-6)-linked and terminal glucoses submitting at the C-4 position every fourteen residues. The biol. activities of GRP upon proliferation of splenic lymphocyte, RAW264.7 cells and A549 cell, and production of nitric oxide (NO) were investigated in vitro. The results showed that GRP exhibited inhibition against A549 cells proliferation and NO production in RAW264.7 cells, and displayed promotion for proliferation of mouse spleen lymphocytes and RAW264.7 cells, which suggested that GRP may have potential immunoregulation, anti-inflammatory and anti-tumor activity.

International Journal of Biological Macromolecules published new progress about Antitumor agents. 59-23-4 belongs to class alcohols-buliding-blocks, name is (2R,3S,4S,5R)-2,3,4,5,6-Pentahydroxyhexanal, and the molecular formula is C6H12O6, Name: (2R,3S,4S,5R)-2,3,4,5,6-Pentahydroxyhexanal.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Liao, Deng-wei published the artcileCharacterization and antitumor activities of polysaccharides obtained from ginger (Zingiber officinale) by different extraction methods, SDS of cas: 59-23-4, the main research area is Zingiber colon breast cervical cancer cell polysaccharide antitumor; Antitumor activity; Ginger polysaccharide; Structure characterization.

Three different extraction technologies including hot water extraction (HWE), enzyme assisted extraction (EAE) and ultrasonic cell grinder extraction (UCGE) were employed to extract crude ginger polysaccharides (GPs) under their resp. best parameters, then crude GPs were purified by DEAE cellulose-52 and Sephadex G-200 size-exclusion chromatog. in that order. Five GPs fractions (HGP, EGP1, EGP2, UGP1, and UGP2, resp.) were obtained. The differences of five GPs in chem. composition, characterization and antitumor activities were further compared. The mol. weights were different in five GPs, varying from 11.81 to 1831.75 kDa. Mannose and glucose as the main monosaccharide and the glycosidic linkage of →4)-α-D-Glc(1→ and -α-Manp-(1→ existed in both five GPs. While EGP2 and UGP1 possessed specific structure of →6)-β-D-Galp-(1→ and UGP1 contained more sulfate group. Moreover, UGP1 exhibited strong inhibitory effect on three tumor cells especially the colon cancer. The inhibition rates of UGP1 on H1975, HCT116 and MCF-7 were 23.339 ± 2.285%, 56.843 ± 2.405% and 21.061 ± 1.920% resp. The study indicated GPs extracted by UCGE could reserve more active structure and inhibit colon cancer more significantly.

International Journal of Biological Macromolecules published new progress about Antitumor agents. 59-23-4 belongs to class alcohols-buliding-blocks, name is (2R,3S,4S,5R)-2,3,4,5,6-Pentahydroxyhexanal, and the molecular formula is C6H12O6, SDS of cas: 59-23-4.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Song, Zilan published the artcileStructure-Activity Relationship Study of Amidobenzimidazole Analogues Leading to Potent and Systemically Administrable Stimulator of Interferon Gene (STING) Agonists, Application of 2,2-Dimethoxyethanamine, the main research area is amidobenzimidazole analog STING agonist SAR immunooncol.

Activation of the stimulator of interferon gene (STING) has emerged as an exciting immuno-oncol. therapeutic strategy; however, the first-generation STING agonists, cyclic dinucleotide (CDN) analogs, have suffered from many disadvantages and failed in clin. trials. Therefore, non-CDN small-mol. STING agonists are urgently needed. In view of the unique structure of the high potency of dimeric amidobenzimidazole STING agonist 5, a structural elaboration was conducted by modifying several structural hotspots of this scaffold. Triazole 40 was identified as a new potent STING activator, possessing EC50 values of 0.24 and 39.51μM for h- and m-STING, resp. This compound has a slightly better pharmacokinetic profile and is >20-fold more aqueously soluble than 5. It activated the STING signaling dramatically by directly binding and stabilizing all h-STING isoforms and m-STING. In vivo, intermittent administration of 40 (I) was found to have significant antitumor efficacy with good tolerance in two mouse tumor models.

Journal of Medicinal Chemistry published new progress about Antitumor agents. 22483-09-6 belongs to class alcohols-buliding-blocks, name is 2,2-Dimethoxyethanamine, and the molecular formula is C4H11NO2, Application of 2,2-Dimethoxyethanamine.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Wu, Chan published the artcileNovel SN38 derivative-based liposome as anticancer prodrug: an in vitro and in vivo study, HPLC of Formula: 111-87-5, the main research area is SN38 PA liposome anticancer; CPT-11; SN38; biodistribution; lipophilic prodrug; long-circulating liposome; pharmacodynamics; pharmacokinetics.

Background: Many novel drug delivery systems have been extensively studied to exploit the full therapeutic potential of SN38, which is one of the most potent antitumor analogs of camptothecins (CPTs), whose clin. application is seriously hindered by poor water solubility, low plasmatic stability, and severe toxicity, but results are always unsatisfactory. Methods: In this study, combining the advantages of prodrug and nanotechnol., a lipophilic prodrug of SN38, SN38-PA, was developed by conjugating palmitic acid to SN38 via ester bond at C10 position, and then the lipophilic prodrug was encapsulated into a long-circulating liposomal carrier by film dispersion method. Results: The SN38-PA liposomes were characterized as follows: an average particle size of 80.13 nm, an average zeta potential of -33.53 mv, and the entrapment efficiency of 99%. Compared with CPT-11, SN38-PA liposome was more stable in close lactone form, more efficient in conversion rate to SN38, and more potent in cytotoxicity against tumor cells. Pharmacokinetic study showed that SN38-PA liposome had significantly enhanced plasma half-life (t1/2) value of SN38 and increased area under the curve (AUC) of SN38, which was 7.5-fold higher than that of CPT-11. Biodistribution study showed that SN38-PA liposome had more active metabolite SN38 in each tissue. Finally, the pharmacodynamic study showed that SN38-PA liposome had higher antitumor effect with the antitumor inhibition rate of 1.61 times than that of CPT-11. Conclusion: These encouraging data merit further investigation on this novel SN38-PA liposome.

International Journal of Nanomedicine published new progress about Antitumor agents. 111-87-5 belongs to class alcohols-buliding-blocks, name is n-Octanol, and the molecular formula is C8H18O, HPLC of Formula: 111-87-5.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Jiang, Xiong-Jie published the artcileA pH-responsive fluorescence probe and photosensitiser based on a tetraamino silicon(IV) phthalocyanine, Recommanded Product: N2-(2-Hydroxyethyl)-N1,N1,N2-trimethyl-1,2-ethylenediamine, the main research area is pH responsive fluorescence probe photosensitizer tetraaminosilicon phthalocyanine.

A novel tetraamino silicon(IV) phthalocyanine has been prepared, of which the fluorescence emission and reactive oxygen species generation efficiency are greatly enhanced at lower pH in the range of ∼5-7, making it a promising pH-controlled and tumor-selective fluorescence probe and photosensitizer for photodynamic therapy.

Chemical Communications (Cambridge, United Kingdom) published new progress about Antitumor agents. 2212-32-0 belongs to class alcohols-buliding-blocks, name is N2-(2-Hydroxyethyl)-N1,N1,N2-trimethyl-1,2-ethylenediamine, and the molecular formula is C7H18N2O, Recommanded Product: N2-(2-Hydroxyethyl)-N1,N1,N2-trimethyl-1,2-ethylenediamine.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Zhang, Jing published the artcileCross-Linked Reverse Vesicle as a General and Effective Vehicle for Hydrophobic Drugs, Quality Control of 7575-23-7, the main research area is crosslinking drug carrier antitumor.

It is well-known that vesicles serve as an excellent delivery platform for hydrophilic drugs. However, there is still a lack of a general and effective platform for hydrophobic drug loading. We herein disclose that water-soluble cross-linked reverse vesicles (cRVs) constructed from anionic surfactant 1, a counterpart of normal vesicles, would be excellent vehicles for hydrophobic drugs, the drug loading content (DLC) for which arrived up to 21.1%, 19.8%, and 25.8%, resp., for three anticancer drugs, paclitaxel, camptothecin, and carmofur. This represents a general drug carrier with high drug loading content for various hydrophobic drugs without the assistance of other external forces. In addition to drug loading superiority, the cRVs were also characterized by robust stability, specific stimulus response, easy postfunctionalization, and good biocompatibility and thus are promising candidates for drug delivery systems.

Langmuir published new progress about Antitumor agents. 7575-23-7 belongs to class alcohols-buliding-blocks, name is Pentaerythritol tetra(3-mercaptopropionate), and the molecular formula is C17H28O8S4, Quality Control of 7575-23-7.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Cho, Er-Chieh published the artcileRing size changes in the development of class I HDAC inhibitors, Category: alcohols-buliding-blocks, the main research area is thienylbenzamide anticancer SAR HDAC inhibitor docking; HDAC; Thienylbenzamides; colon cancer; ring transformation.

Five pathways involving different ring structures led to generation of fourteen thienylbenzamides which display the structure-activity relationships of class I HDAC inhibitors. All the synthesized compounds inhibit HDAC1 and HDAC2 selectively over other isoforms and many inhibit DLD1 and HCT116 cells more effectively than a parent compound Compounds and inhibit HCT116 cells by activation of the apoptosis pathway.

Journal of Enzyme Inhibition and Medicinal Chemistry published new progress about Antitumor agents. 22483-09-6 belongs to class alcohols-buliding-blocks, name is 2,2-Dimethoxyethanamine, and the molecular formula is C4H11NO2, Category: alcohols-buliding-blocks.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Wang, Zichao published the artcileEfficient biosynthesis of anticancer polysaccharide by a mutant Chaetomium globosum ALE20 via non-sterilized fermentation, Formula: C6H12O6, the main research area is fermentation Chaetomium globosum polysaccharide batch fermentation; Adaptive laboratory evolution; Anticancer polysaccharide; Methanol-resistant strain.

The sterilization process, due to its immense energy consumption, high facilities investment, and loss of raw materials by caramelization, during industrial production has drawn much attention. In this study, a methanol-resistant mutant strain, Chaetomium globosum ALE20, was obtained following 20 cycles of adaptive laboratory evolution process. The titer of anticancer polysaccharide (GCP-M) from C. globosum ALE20 reached 9.2 g/L with glycerol as sole carbon source using non-sterilized and fed-batch fermentation strategy. This titer represents a 200% increase compared with the 3.3 g/L attained with batch fermentation The GCP-M monosaccharide was comprised of galactose, glucose, mannose and glucuronic acid, in a molar ratio of 3.83:66.37:3.26:1.95, resp., and its weight-average mol. weight and polydispersity were 3.796 × 104 Da and 1.060, resp. This work presents an ideal alternative and safer fermentation process without sterilization, and a useful approach for enhancing industrial production

International Journal of Biological Macromolecules published new progress about Antitumor agents. 59-23-4 belongs to class alcohols-buliding-blocks, name is (2R,3S,4S,5R)-2,3,4,5,6-Pentahydroxyhexanal, and the molecular formula is C6H12O6, Formula: C6H12O6.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts