Tag: M.W=150-200

Vidic, Jasmina Minic published the artcileQuantitative assessment of olfactory receptors activity in immobilized nanosomes: a novel concept for bioelectronic nose, Synthetic Route of 1205-17-0, the main research area is olfactory receptor immobilization nanosome bioelectronic nose.

The authors describe how mammalian olfactory receptors (ORs) could be used as sensing elements of highly specific and sensitive bioelectronic noses. An OR and an appropriate Gα protein were co-expressed in Saccharomyces cerevisiae cells from which membrane nanosomes were prepared, and immobilized on a sensor chip. By Surface Plasmon Resonance, the authors were able to quant. evaluate OR stimulation by an odorant, and G protein activation. The authors demonstrate that ORs in nanosomes discriminate between odorant ligands and unrelated odorants, as in whole cells. This assay also provides the possibility for quant. assessment of the coupling efficiency of the OR with different Gα subunits, without the interference of the cellular transduction pathway. The authors’ findings will be useful to develop a new generation of electronic noses for detection and discrimination of volatile compounds, particularly amenable to micro- and nano-sensor formats.

Lab on a Chip published new progress about Alkyl groups. 1205-17-0 belongs to class isoquinoline, name is 2-Methyl-3-(3,4-methylenedioxyphenyl)propionaldehyde, and the molecular formula is C11H12O3, Synthetic Route of 1205-17-0.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Yuan, Xu published the artcileDesign, synthesis and in vitro evaluation of 6-amide-2-aryl benzoxazole/benzimidazole derivatives against tumor cells by inhibiting VEGFR-2 kinase, Computed Properties of 104-01-8, the main research area is amide aryl benzoxazole preparation antitumor antiangiogenesis VEGFR2 tyrosine kinase; benzimidazole amide aryl preparation antitumor antiangiogenesis VEGFR2 tyrosine kinase; Angiogenesis; Antitumor activity; Benzimidazole; Benzoxazole; VEGFR-2.

A library of thirty-seven 6-amide-2-aryl benzoxazoles I (R1 = H, F, Br, Cl and MeO; R2 = F, Br, Cl, Me and MeO; R3 = H and MeO; X = O; X1 = H and Cl; X2 = H, 2-F, 2-Cl, 2-Br and 3-Br; n = 0, 1)/benzimidazoles I (R1 = H, F, Br and MeO; R2 = Cl, Me and MeO; R3 = H and MeO; R3 = Cl, Me and OMe; X = NH; X1 = Cl; X2 = H; n = 0, 1) has been designed and synthesized based on the highly conserved active site of VEGFR-2. Several title compounds I exhibited selective inhibitory activities against VEGFR-2 than EGFR kinases, which also displayed selective anti-proliferation potency against the HUVEC and HepG2 than the A549 and MDA-MB-231 cancer cell lines. The newly synthesized compounds I were evaluated for anti-angiogenesis capability by chick chorioallantoic membrane (CAM) assay. Among them, compounds I (R1 = R3 = H; R2 = OMe; n = 1; X = NH; X1 = Cl; X2 = H) showed the most potent anti-angiogenesis ability (79% inhibition at 10 nM/eggs), the efficient cytotoxic activities (in vitro against the HUVEC and HepG2 cell lines with IC50 values of 1.47 and 2.57 μM, resp.), and excellent VEGFR-2 kinase inhibition (IC50 = 0.051 μM). The mol. docking anal. revealed that compound I (R1 = R3 = H; R2 = OMe; n = 1; X = NH; X1 = Cl; X2 = H) is a Type II inhibitor of VEGFR-2 kinase. These results indicated that the 6-amide-2-arylbenzoxazoles and 6-amide-2-aryl benzimidazoles I are promising inhibitors of VEGFR-2 kinase for the potential treatment of anti-angiogenesis.

European Journal of Medicinal Chemistry published new progress about Angiogenesis. 104-01-8 belongs to class isoquinoline, name is 4-Methoxyphenylacetic acid, and the molecular formula is C9H10O3, Computed Properties of 104-01-8.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Wang, Cong published the artcileDiscovery of chalcone-modified estradiol analogs as antitumour agents that Inhibit tumour angiogenesis and epithelial to mesenchymal transition, Name: 2,3-Dimethoxybenzaldehyde, the main research area is estradiol chalcone analog preparation antitumor antiangiogenic; 2-Methoxyestradiol; Angiogenesis; Antitumour; EMT; Migration.

Angiogenesis plays an essential role in tumorigenesis and tumor progression, and anti-angiogenesis therapies have shown promising antitumor effects in solid tumors. 2-Methoxyestradiol (2ME2), an endogenous metabolite of estradiol, has been regarded as a potential antitumor agent mainly targeting angiogenesis. Here we synthesized a novel series of chalcones based on 2-methoxyestradiol and evaluated their potential activities against tumors. Compound I was demonstrated to have potent antiangiogenic activity. Further studies showed that I suppressed tumor growth in human breast cancer (MCF-7) xenograft models without obvious side effects. Evaluation of the mechanism revealed that I targeted the epithelial to mesenchymal transition (EMT) process in MCF-7 cells and inhibited HUVEC migration and then contributed to hindrance of angiogenesis. Thus, I may be a promising antitumor agent with excellent efficacy and low toxicity.

European Journal of Medicinal Chemistry published new progress about Angiogenesis. 86-51-1 belongs to class isoquinoline, name is 2,3-Dimethoxybenzaldehyde, and the molecular formula is C9H10O3, Name: 2,3-Dimethoxybenzaldehyde.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Smirnova, Irina published the artcileHollongdione arylidene derivatives induce antiproliferative activity against melanoma and breast cancer through pro-apoptotic and antiangiogenic mechanisms, Application of 2,3-Dimethoxybenzaldehyde, the main research area is melanoma breast cancer hollongdione arylidene derivative antiangiogensis; Antiproliferative activity; Arylidene; CAM assay; Claisen-Schmidt aldol condensation; Cytotoxicity; Dammarane triterpenoids; Dipterocarpol; Hollongdione; NCI-60; rtPCR.

The use of natural compounds as starting point for semisynthetic derivatives has already been proven as a valuable source of active anticancer agents. Hollongdione (4,4,8,14-tetramethyl-18-norpregnan-3,20-dion), obtained by few steps from dammarane type triterpenoid dipterocarpol, was chem. modified at C2 and C21 carbon atoms by the Claisen-Schmidt aldol condensation to give a series of arylidene derivatives The anticancer activity of the obtained compounds was assessed on NCI-60 cancer cell panel, revealing strong antiproliferative effects against a large variety of cancer cells. 2,21-Bis-[3-pyridinyl]-methylidenohollongdione 9 emerged as the most active derivative as indicated by its GI50 values in the micromolar range which, combined with its high selectivity index values, indicated its suitability for deeper biol. investigation. The mechanisms involved in compound 9 antiproliferative activity, were investigated through in vitro (DAPI staining) and ex vivo (CAM assay) tests, which exhibited its apoptotic and antiangiogenic activities. In addition, compound 9 showed an overall inhibition of mitochondrial respiration. rtPCR anal. identified the more intimate activity at pro-survival/pro-apoptotic gene level. Collectively, the hollongdione derivative stand as a promising therapeutic option against melanoma and breast cancer provided that future in vivo anal. will certify its clin. efficacy.

Bioorganic Chemistry published new progress about Angiogenesis. 86-51-1 belongs to class isoquinoline, name is 2,3-Dimethoxybenzaldehyde, and the molecular formula is C9H10O3, Application of 2,3-Dimethoxybenzaldehyde.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Bhagat, Kavita published the artcileMicrowave-assisted synthesis of 11-substituted-3,3-dimethyl-2,3,4,5,10,11-hexahydrodibenzo[b,e][1,4]diazepin-1-one derivatives catalysed by silica supported fluoroboric acid as potent antioxidant and anxiolytic agents, Recommanded Product: 2,3-Dimethoxybenzaldehyde, the main research area is dimethyl hexahydrodibenzodiazepinone preparation antioxidant anxiolytic activity green chem; phenylenediamine dimedone aldehyde fluoroboric acid catalyst cyclocondensation microwave irradiation.

A novel series of benzodiazepine derivatives I [R = Ph, 4-chlorophenyl, 4-bromophenyl, etc.] as antioxidant and anxiolytic agents were synthesized. All the compounds were obtained in good yield by facile synthesis. To check their antioxidant potential, DPPH (2,2-diphenyl-1-picrylhydrazyl) free radical scavenging assay was performed. Among all the synthetics seven derivatives I [R = 3-methoxyphenyl, 4-nitrophenyl, 3-methyl-2-thienyl, cinnamyl, 1-naphthyl 3,4-dichlorophenyl, 3-bromophenyl] exhibited IC50 values ranging from 76 to 489 nM. These seven compounds were further evaluated to check their binding abilities towards the benzodiazepine binding site on GABAA receptors. Three best-fit ligands I [R = 3-methoxyphenyl, 1-naphthyl, 3,4-dichlorophenyl] were further evaluated for their anxiolytic effect by using three in-vivo mice models i.e. Elevated Plus Maze, Light & Dark box, and Mirror Chamber model. The study revealed that compounds I [R = 3,4-dichlorophenyl, 1-naphthyl] showed the best anxiolytic effect as compared to standard drug diazepam even at an oral dose of 1.0 mg/kg.

Medicinal Chemistry Research published new progress about Antioxidants. 86-51-1 belongs to class isoquinoline, name is 2,3-Dimethoxybenzaldehyde, and the molecular formula is C9H10O3, Recommanded Product: 2,3-Dimethoxybenzaldehyde.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Jerkovic, I. published the artcileContribution to the characterisation of honey-based Sardinian product abbamele: Volatile aroma composition, honey marker compounds and antioxidant activity, Recommanded Product: 5-Methyl-2-phenylhex-2-enal, the main research area is honey abbamele aroma marker antioxidant.

Sardinian abbamele is a typical product obtained from the honey recuperation from combs (traditional procedure) or by concentration of the honey diluted in water (industrial procedure). Seven abbamele samples were obtained to study the volatiles’ composition, the presence of honey marker compounds and their relationship with the production procedures. The long thermal treatment applied in abbamele production caused very high (1007.0-4405.8 mg/kg) HMF content (HPLC-DAD), while glucose and fructose amounts were quite similar to the honey ones (HPLC-RI). Total antioxidant activity (FRAP assay) of the samples ranged between 13.3 and 71.2 mmol Fe2+/kg, while antiradical activity (DPPH assay) ranged between 3.8 and 23.3 mmol TEAC/kg. Such high antioxidant values were linearly correlated with total phenol amount (1297.8-4469.5 mg GAE/kg) determined by Folin-Ciocalteau method. Thermally derived furan derivatives and terpenes were abundant among the headspace volatiles (HS-SPME), particularly limonene (0.5-76.0%) that probably originated from citrus rinds’ addition during abbamele production GC and GC-MS analyses of USE isolates revealed HMF predominance as well as the honey marker compounds (if/when existing) such as Me syringate (up to 49.2%), marker of Asphodelus microcarpus honey. High isophorone percentage (up to 30.9%) determined by HS-SPME followed by minor percentage of 4-ketoisophorone and norisoprenoids in one sample indicated Arbutus unedo L. honey use in the production HPLC-DAD anal. confirmed the presence of specific honey markers: two samples showed high Me syringate concentrations (150.4-120.1 mg/kg) while homogentisic acid and other specific markers of A. unedo honey were found in one sample. The compared GC-MS and HPLC-DAD data proved to be useful to obtain information about the use of specific honey in the production and to verify citrus addition

Food Chemistry published new progress about Antioxidants. 21834-92-4 belongs to class isoquinoline, name is 5-Methyl-2-phenylhex-2-enal, and the molecular formula is C13H16O, Recommanded Product: 5-Methyl-2-phenylhex-2-enal.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Chandrashekhara, S. published the artcileThiazolidin-4-one derivatives on human lung fibroblast shows oxygen free radical scavenging activity, Formula: C9H10O3, the main research area is thiazolidinone benzylidenehydrazono preparation antioxidant human.

In present study, a more chem. versatile and diverse thiazolidin-4-one derivatives I (R = Ph, 4-ClC6H4, 2-thienyl, etc.) were synthesized as suitable pharmacophores for antioxidant activity. Antioxidant activity was evaluated by using both enzymic and non-enzymic activities such as catalase (CAT), superoxide dismutase (SOD), glutathione peroxidase (GPX) on cell lines and free radical scavenging activity by DPPH (1,1-diphenyl-2-picrylhydrazine) assay method and ferric reducing antioxidant power (FRAP) assays. All tested compounds exhibited excellent antioxidant activity. In addition, all the synthesized derivatives showed non-toxic effects against a diseased human lung fibroblast (COPD), HCC7231 (TACC CCL-96). In prospect study, the movement of the compounds may be manipulated by optimizing a lead mol. by introducing unsaturation or heterocyclic ring at C5 of thiazolidinediones. The outcomes of such studies may be pos. for the clin. applications in humans and may open up a new therapeutic avenue.

International Research Journal of Pharmacy published new progress about Antioxidants. 86-51-1 belongs to class isoquinoline, name is 2,3-Dimethoxybenzaldehyde, and the molecular formula is C9H10O3, Formula: C9H10O3.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Gusain, Anamika published the artcileAntiradical Properties of trans-2-(4-substituted-styryl)-thiophene, Computed Properties of 104-01-8, the main research area is trans substituted styryl thiophene antiradical property fluorescence DFT study; Absorption; Antioxidant ability; Bond dissociation energy; Density functional theory; Fluorescence; Ionization energy; Phenol; Proton affinity; Stilbene; Thiophene.

2-Substituted thiophene compounds with electron donating and electron withdrawing p-Ph substitution were synthesized and studied their radical scavenging properties using DPPH assay and DFT method. It is shown that p-hydroxy and p-amino Ph substituted compound exhibit radical scavenging activity. From DFT and radical scavenging studies, a correlation between IC50 with the bond dissociation enthalpy, proton affinity, ground state dipole moment and optical band gap of compound is found. Compounds 1-3 with electron withdrawing substituent (NO2, CN, Cl) do not show any radical scavenging properties, whereas compounds 6-7 with electron donating substituent (OH, NH2) show antiradical properties. Further, the antiradical activity is reduced drastically by replacing the -OH and -NH2 with methoxy and -N-alkylating group resp. in 6 and 7. The compound with p-hydroxy Ph substitution, exhibits stronger antiradical activity as compared to the p-amino Ph substitution due to smaller O-H bond dissociation energy as compared to the N-H bond. From DPPH and DFT studies, it is suggested that the radical scavenging activity in 2-substituted thiophene is occurred through proton transfer mechanism. The other possible SET, SPLET mechanisms are also corroborated.

Journal of Fluorescence published new progress about Antioxidants. 104-01-8 belongs to class isoquinoline, name is 4-Methoxyphenylacetic acid, and the molecular formula is C9H10O3, Computed Properties of 104-01-8.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Kumar, Jagdeep published the artcileAntioxidant properties of ethenyl indole: DPPH assay and TDDFT studies, Recommanded Product: 4-Methoxyphenylacetic acid, the main research area is phenylethenyl indole preparation antioxidant ionization potential UV spectra.

A series of ethenyl indoles (e.g. 3-(4-substituted phenylethenyl-E)-N-H-indole) with various donor or acceptor substituents have been synthesized and their antioxidant properties have been studied. Ethenyl indoles exhibit antioxidant activity in a substituent dependent manner. Ethenyls bearing strong electron withdrawing substituents show weak or no antioxidant activity, whereas ethenyls with electron donating substituents exhibit antioxidant properties comparable to vitamin E. It can be seen from a plot of the percentage of inhibition vs. the antioxidant concentration, that the hydroxy substituted ethenyl indole exhibits good antioxidant properties (50% inhibition concentration (IC50) âˆ?24μM) as compared to the other ethenyls (IC50: 30-63μM) and that it is comparable to vitamin E (IC50 âˆ?26μM). The results are also supported by the computational data obtained through time dependent d. functional theory (TDDFT) calculations From the TDDFT and antioxidant study, it was shown that there is a correlation between the HOMO-LUMO energy, the ground state dipole moment, optical band gap, bond dissociation enthalpy and the ionization potential of the ethenyls with the antioxidant properties. A possible hydrogen and/or electron and proton transfer mechanism is suggested for the quenching of the free radical.

New Journal of Chemistry published new progress about Antioxidants. 104-01-8 belongs to class isoquinoline, name is 4-Methoxyphenylacetic acid, and the molecular formula is C9H10O3, Recommanded Product: 4-Methoxyphenylacetic acid.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Popova, Svetlana A. published the artcileIsobornylchalcones as scaffold for the synthesis of diarylpyrazolines with antioxidant activity, Related Products of isoquinoline, the main research area is diarylpyrazoline isobornylchalcone scaffold antioxidant activity; Fe2+/ascorbate-initiated lipid peroxidation; antioxidant activity; diarylpyrazolines; isobornylchalcones.

The pyrazoline ring is defined as a “”privileged structure”” in medicinal chem. A variety of pharmacol. properties of pyrazolines is associated with the nature and position of various substituents, which is especially evident in diarylpyrazolines. Compounds with a chalcone fragment show a wide range of biol. properties as well as high reactivity which is primarily due to the presence of an α, β-unsaturated carbonyl system. At the same time, bicyclic monoterpenoids deserve special attention as a source of a key structural block or as one of the pharmacophore components of biol. active mols. A series of new diarylpyrazoline derivatives based on isobornylchalcones with different substitutes (MeO, Hal, NO2, N(Me)2) was synthesized. Antioxidant properties of the obtained compounds were comparatively evaluated using in vitro model Fe2+/ascorbate-initiated lipid peroxidation in the substrate containing brain lipids of laboratory mice. It was demonstrated that the combination of the electron-donating group in the para-position of ring B and OH-group in the ring A in the structure of chalcone fragment provides significant antioxidant activity of synthesized diarylpyrazoline derivatives

Molecules published new progress about Antioxidants. 86-51-1 belongs to class isoquinoline, name is 2,3-Dimethoxybenzaldehyde, and the molecular formula is C9H10O3, Related Products of isoquinoline.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem