Month: November 2022

Hong, Seunghee published the artcileDiscovery of new azaindole-based PI3Kα inhibitors: Apoptotic and antiangiogenic effect on cancer cells, Formula: C13H8BrIN2O2S, the publication is Bioorganic & Medicinal Chemistry Letters (2010), 20(24), 7212-7215, database is CAplus and MEDLINE.

Phosphatidylinositol-3-kinase alpha (PI3Kα) is an important target in cancer due to the deregulation of the PI3K/AKT signaling pathway in many tumors. In this study, we designed [3,5-d]-7-azaindole analogs as PI3Kα inhibitors through the fragment-growing strategy. By varying groups at the 3,5-positions of azaindole, we developed the SAR (Structure-activity relationship) and identified a series of potent PI3Kα inhibitors. Representative azaindole derivatives showed activity in a cellular proliferation and apoptosis assays. Moreover, I exhibited strong antiangiogenic effects on cancer cells.

Bioorganic & Medicinal Chemistry Letters published new progress about 757978-19-1. 757978-19-1 belongs to iodides-buliding-blocks, auxiliary class Other Aromatic Heterocyclic,Bromide,Iodide,Sulfamide,Benzene, name is 5-Bromo-3-iodo-1-(phenylsulfonyl)-1H-pyrrolo[2,3-b]pyridine, and the molecular formula is C13H8BrIN2O2S, Formula: C13H8BrIN2O2S.

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

Tsang, Chui-Shan published the artcileUnexpected Promotional Effects of Alkyl-Tailed Ligands and Anions on the Electrochemical Generation of Ruthenium(IV)-Oxo Complexes, SDS of cas: 638-45-9, the publication is ChemElectroChem (2021), 8(12), 2221-2230, database is CAplus.

Electro-generation of Ru^IV=O species from the RuII-aqua complex is a crucial step to excel the electrocatalytic water oxidation performance of ruthenium oxo complexes. We report herein the synthesis and X-ray crystal structural characterizations of new RuII-aqua complexes containing N-substituted 2,2′-dipyridylamine ligands (L) tagged with an alkyl chain of various lengths, [Ru(tpy)(L)(OH₂)]²⁺. Cyclic voltammetric analyses show that the length of the alkyl chain exerts great influence on the electro-generation of Ru^IV=O species. The L with a longer alkyl chain in an acidic aqueous medium promotes the conversion of Ru^III-OH to Ru^IV=O efficiently. Surprisingly, this conversion can be further enhanced by the presence of perchlorate anions. Chronocoulometric data reveal that the alkyl chain on L promotes the adsorption of the ruthenium complex on the electrode surface. Bulk electrolysis results indicate that the [Ru(tpy)(dppa)(OH₂)]²⁺ (dppa=(2,2′-dipyridyl)-n-propylamine) gives the most active electrocatalytic water oxidation activity among the ruthenium-aqua complexes investigated in this study.

ChemElectroChem published new progress about 638-45-9. 638-45-9 belongs to iodides-buliding-blocks, auxiliary class Iodide,Aliphatic hydrocarbon chain, name is 1-Iodohexane, and the molecular formula is C10H10O2, SDS of cas: 638-45-9.

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

Lee, Soyoung published the artcileDevelopment and Biological Evaluation of Potent and Selective c-KIT^D816V Inhibitors, Quality Control of 757978-19-1, the publication is Journal of Medicinal Chemistry (2014), 57(15), 6428-6443, database is CAplus and MEDLINE.

The c-KIT tyrosine kinase has emerged as a potential therapeutic target for an array of diseases. However, there exists a drug resistance that is caused by mutations in c-KIT; therefore, c-KIT remains as a clin. challenge due to limited effective treatment options for therapies. For example, the acquired activating point mutation D816V significantly impairs the efficacy of targeted cancer therapies. Understanding the mechanisms of drug resistance at the mol. level will aid in designing and developing particular inhibitors with the potential to overcome these resistance mutations. The authors undertake a structure-based de novo design of 7-azaindole as the mol. core using the modified scoring function. This approach led to an identification of new c-KIT inhibitors over 100-fold specific for the D816V mutant relative to the wild-type c-KIT with nanomolar inhibitory activity. More importantly, these compounds potently inhibit clin. relevant D816V mutations of c-KIT in biochem. and cellular studies.

Journal of Medicinal Chemistry published new progress about 757978-19-1. 757978-19-1 belongs to iodides-buliding-blocks, auxiliary class Other Aromatic Heterocyclic,Bromide,Iodide,Sulfamide,Benzene, name is 5-Bromo-3-iodo-1-(phenylsulfonyl)-1H-pyrrolo[2,3-b]pyridine, and the molecular formula is C13H8BrIN2O2S, Quality Control of 757978-19-1.

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

Ahn, Jin Hee published the artcileA new synthesis of γ-dialkoxy carboxylic acid derivatives via radical coupling reaction of α-halo acid derivatives with vinyl ethers, Formula: C5H9IO2, the publication is Synlett (1996), 1224-1226, database is CAplus.

γ-Dialkoxy carboxylic acid derivatives were prepared conveniently by the radical coupling reaction of α-halo carboxylic acid derivatives with vinyl ethers in 65-95% yield using Ni₂B(cat.)-BER in MeOH in the presence of NaI.

Synlett published new progress about 31253-08-4. 31253-08-4 belongs to iodides-buliding-blocks, auxiliary class Iodide,Ester, name is Ethyl 2-Iodopropionate, and the molecular formula is C5H9IO2, Formula: C5H9IO2.

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

Gaux, Bernard published the artcilePartial deiodination of polyiodo compounds with lithium aluminum hydride, COA of Formula: C7H8INO, the publication is Bulletin de la Societe Chimique de France (1974), 505-9, database is CAplus.

Triiodobenzoic acids reacted with LiAlH4 to give the resp. diiodobenzyl alcs. 3,5-Diiodanthranilic and -salicylic acids gave the resp. diiodobenzyl alcs. as well as monoiodobenzyl alcs. 4-Amino-3,5-diioidobenzoic acid gave only 3,5,4-I2(H2N)-C6H2CH2OH.

Bulletin de la Societe Chimique de France published new progress about 53279-83-7. 53279-83-7 belongs to iodides-buliding-blocks, auxiliary class Iodide,Amine,Benzene,Alcohol, name is (2-Amino-5-iodophenyl)methanol, and the molecular formula is C7H8INO, COA of Formula: C7H8INO.

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

Kindt, Nadege published the artcilePharmacological inhibition of macrophage migration inhibitory factor interferes with the proliferation and invasiveness of squamous carcinoma cells, HPLC of Formula: 41270-96-6, the publication is International Journal of Oncology (2013), 43(1), 185-193, database is CAplus and MEDLINE.

Recent clin. observations and exptl. studies of our group indicate that macrophage migration inhibitory factor (MIF) may contribute to tumor progression in head and neck squamous cell carcinomas (HNSCC). The present study was undertaken to examine the effects of the irreversible MIF inhibitor 4-iodo-6-phenylpyrimidine (4-IPP) on proliferation and invasiveness of the squamous carcinoma cell line SCCVII. Cell counting, crystal violet assay and flow cytometry were used to analyze the effects of 4-IPP on SCCVII cell growth. The impact of 4-IPP on cell invasiveness was assessed by Boyden chamber assay. Knockdown of the MIF receptor CD74 was achieved by transduction with lentiviral vectors encoding anti-CD74 shRNAs. As shown by immunofluorescence staining, SCCVII cells express both MIF and CD74. Decreased MIF immunoreactivity as a result of exposure to 4-IPP suggested a covalent modification of the cytokine. 4-IPP inhibited SCCVII cell proliferation and invasiveness. Moreover, the cytostatic effect of 4-IPP was enhanced by CD74 knockdown. The inhibitory effects of 4-IPP on cell proliferation and invasiveness strongly suggest that MIF is involved in proliferative activity and invasive properties of squamous carcinoma cells. In conclusion, MIF inhibition may open possibilities for target-directed treatment of head and neck squamous cell carcinoma.

International Journal of Oncology published new progress about 41270-96-6. 41270-96-6 belongs to iodides-buliding-blocks, auxiliary class Pyrimidine,Iodide,Benzene,Immunology/Inflammation,MIF, name is 4-Iodo-6-phenylpyrimidine, and the molecular formula is C10H7IN2, HPLC of Formula: 41270-96-6.

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

Poleshchuk, O. Kh. published the artcileStudy of the electronic structure of the ICl·Py complex, Recommanded Product: Pyridine Iodochloride complex, the publication is Russian Journal of Coordination Chemistry (Translation of Koordinatsionnaya Khimiya) (1998), 24(1), 67-71, database is CAplus.

The results of ab initio and semiempirical calculations are used to analyze the frequency changes in the NQR, X-ray fluorescence, and photoelectron spectra of the ICl·Py complex. A comparison of the calculated MO energies with the exptl. ionization potentials made it possible to explain the stability of the complex. The results obtained are used to elucidate the origin of the complexation-induced chlorine, iodine, and nitrogen NQR frequency shifts.

Russian Journal of Coordination Chemistry (Translation of Koordinatsionnaya Khimiya) published new progress about 6443-90-9. 6443-90-9 belongs to iodides-buliding-blocks, auxiliary class Pyridines, name is Pyridine Iodochloride complex, and the molecular formula is C5H5ClIN, Recommanded Product: Pyridine Iodochloride complex.

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

Tahmouresilerd, Babak published the artcileMake room for iodine: systematic pore tuning of multivariate metal-organic frameworks for the catalytic oxidation of hydroquinones using hypervalent iodine, Recommanded Product: Dimethyl 2-iodoterephthalate, the publication is Catalysis Science & Technology (2018), 8(17), 4349-4357, database is CAplus.

Iodine sites have been incorporated in both MIL-53 (Al) and UiO-66 (Zr) MOFs. A multivariate approach was used to increase the accessible area within the pores to allow for the catalytic oxidation of a model substrate, hydroquinone, to the corresponding quinone. In the process, three new phases of MIL-53 were discovered, one of which proved instrumental in allowing catalysis to occur. Both UiO-66 and MIL-53 with 25% incorporated iodine containing linkers allowed for a near-ideal balance between high d. of catalytic sites and sufficient space for mass transport to enable catalysis to occur. Good conversions and selectivities were observed in nitromethane, Et acetate, acetone and ethanol with UiO-66 which proved to be the more active of the two catalysts. Oxone and 3-chloroperbenzoic acid acted as competent cooxidants. XPS revealed that the reaction proceeded through an I(III) oxidation state. The MIL-53 framework was readily recycled while the UiO-66 MOF suffered from catalyst deactivation due to particle agglomeration. UiO-66 with 25% iodine containing linker proved to be a competent catalyst for a variety of substituted hydroquinones.

Catalysis Science & Technology published new progress about 165534-79-2. 165534-79-2 belongs to iodides-buliding-blocks, auxiliary class Iodide,Benzene,Ester, name is Dimethyl 2-iodoterephthalate, and the molecular formula is C12H14IN, Recommanded Product: Dimethyl 2-iodoterephthalate.

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

Hammarlund, E. R. published the artcileMethods of preparing isotonic solutions by means of graphs or tables on the basis of experimentally found iso-osmotic values, Computed Properties of 101-29-1, the publication is Pharmaceutica Acta Helvetiae (1960), 593-607, database is CAplus.

Four graphical and three tabular methods for preparing isotonic aqueous solutions are described. New exptl. data is presented for 353 compounds to be used for the recommended and most practical of the methods studied for isotonicity adjustment. All the methods described may be used in practical pharmacy. The graphical methods are more accurate but consume more space than the tabular methods.

Pharmaceutica Acta Helvetiae published new progress about 101-29-1. 101-29-1 belongs to iodides-buliding-blocks, auxiliary class Pyridine,Iodide,Carboxylic acid,Ketone, name is 2-(3,5-Diiodo-4-oxopyridin-1(4H)-yl)acetic acid, and the molecular formula is C7H5I2NO3, Computed Properties of 101-29-1.

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

Yao, Tuanli published the artcileSynthesis of Isocoumarins and α-Pyrones via Electrophilic Cyclization, Safety of Dimethyl 2-iodoterephthalate, the publication is Journal of Organic Chemistry (2003), 68(15), 5936-5942, database is CAplus and MEDLINE.

A variety of substituted isocoumarins, e.g. I [R¹ = H, MeO; R² = H, MeO, MeO₂C; R³ = HO(CH₂)₃, Ph, n-hexyl, etc.; R⁴ = H, iodo, 4-O₂NC₆H₄S, PhSe], and α-pyrones, e.g. II [R⁵ = H, Me, Ph; R⁶ = H, Ph; R⁵R⁶ = (CH₂)₃; R⁷ = Bu, Ph], are readily prepared in excellent yields under very mild reaction conditions by the reaction of o-(1-alkynyl)benzoates, e.g. III (R⁸ = Me, Me₃C), or (Z)-2-alken-4-ynoates, e.g. IV (R⁹ = Me, Et), resp., with ICl, I₂, PhSeCl, p-O₂NC₆H₄SCl, and hydrogen iodide. This methodol. accommodates various alkynyl esters and has been successfully extended to the synthesis of polycyclic aromatic and biaryl compounds

Journal of Organic Chemistry published new progress about 165534-79-2. 165534-79-2 belongs to iodides-buliding-blocks, auxiliary class Iodide,Benzene,Ester, name is Dimethyl 2-iodoterephthalate, and the molecular formula is C27H39ClN2, Safety of Dimethyl 2-iodoterephthalate.

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