Tag: 167.0012

eCF309: a potent, selective and cell-permeable mTOR inhibitor was written by Fraser, Craig;Carragher, Neil O.;Unciti-Broceta, Asier. And the article was included in MedChemComm in 2016.COA of Formula: C4H7BrO2 This article mentions the following:

Kinase inhibitors capable of blocking the phosphorylation of protein substrates with high selectivity are essential to probe and elucidate the etiol. role of such mols. and their signalling pathways. By addressing these biochem. questions in disease relevant cell-based and in vivo models, strong pharmacol. evidence can be generated towards validating or disproving a target hypothesis. Pharmacol. studies can also provide fundamental information to identify appropriate biomarkers and rational drug combination strategies and thereby facilitate clin. translation. However, due to the high number of kinases encoded by the human genome (>500) and their highly conserved catalytic domains, the development of such an elite class of inhibitors-a.k.a. high-quality chem. probes-represents a major challenge. Through a ligand-based inhibitor design, focused library synthesis and phenotypic screening to prioritize compounds with potent cell activity, we recently identified a cell cycle inhibitor with micromolar potency that inhibits mTOR kinase activity. Following a rapid lead optimization campaign, we report the development of eCF309, an mTOR inhibitor displaying low nanomolar potency both in vitro and in cells and an excellent selectivity profile (S-score (35%) = 0.01 at 10 μM). In the experiment, the researchers used many compounds, for example, 2-Bromomethyl-1,3-dioxolane (cas: 4360-63-8COA of Formula: C4H7BrO2).

2-Bromomethyl-1,3-dioxolane (cas: 4360-63-8) belongs to dioxole derivatives. Dioxoles, particularly fluorinated dioxoles, are used as co-monomers to make polymers that find use in forming protective coatings for chemical resistance. 1,3-Benzodioxole can be synthesized from catechol with disubstituted halomethanes.COA of Formula: C4H7BrO2

Referemce:
1,3-Benzodioxole – Wikipedia,
Dioxole | C3H4O2 – PubChem

Synthetic study of marine diterpenoid aberrarone: stereocontrolled construction of tetracyclic framework was written by Kobayashi, Toyoharu;Tokumoto, Kasumi;Tsuchitani, Yuki;Abe, Hideki;Ito, Hisanaka. And the article was included in Tetrahedron in 2015.Recommanded Product: 2-Bromomethyl-1,3-dioxolane This article mentions the following:

Highly stereocontrolled synthesis of the tetracyclic framework of the marine diterpenoid aberrarone (I), which possesses antimalarial activity against a chloroquine-resistant strain of Plasmodium, has been accomplished. A key feature of the synthesis is the complete stereocontrolled construction of C- and D-ring using stereoselective 1,4-addition followed by intramol. aldol reaction protocol. In the experiment, the researchers used many compounds, for example, 2-Bromomethyl-1,3-dioxolane (cas: 4360-63-8Recommanded Product: 2-Bromomethyl-1,3-dioxolane).

2-Bromomethyl-1,3-dioxolane (cas: 4360-63-8) belongs to dioxole derivatives. Dioxoles, particularly fluorinated dioxoles, are used as co-monomers to make polymers that find use in forming protective coatings for chemical resistance. Dioxole functionalized metal-organic frameworks have also been recently reported.Recommanded Product: 2-Bromomethyl-1,3-dioxolane

Referemce:
1,3-Benzodioxole – Wikipedia,
Dioxole | C3H4O2 – PubChem

Synthesis and Unexpected Transformation of 5-[(1,3-Dioxolan-2-ylmethyl)sulfanyl]-1H-pyrrol-2-amine into 5-{[2-(2-Hydroxyethoxy)ethenyl]sulfanyl}-1H-pyrrol-2-amine in the Presence of a Superbase was written by Nedolya, N. A.;Tarasova, O. A.;Albanov, A. I.;Trofimov, B. A.. And the article was included in Russian Journal of Organic Chemistry in 2021.Category: dioxole This article mentions the following:

Successive one-pot reactions of monolithiated N,N-diethylprop-2-yn-1-amine with 2-(ethenyloxy)ethyl isothiocyanate and 2-(bromomethyl)-1,3-dioxolane afforded I in 91% yield. In the system t-BuOK-DMSO at room temperature (1 h), the product was converted to E/Z-II (yield 68%) instead of expected 1-vinyl derivative In the experiment, the researchers used many compounds, for example, 2-Bromomethyl-1,3-dioxolane (cas: 4360-63-8Category: dioxole).

2-Bromomethyl-1,3-dioxolane (cas: 4360-63-8) belongs to dioxole derivatives. Dioxoles, particularly fluorinated dioxoles, are used as co-monomers to make polymers that find use in forming protective coatings for chemical resistance. Dioxole functionalized metal-organic frameworks have also been recently reported.Category: dioxole

Referemce:
1,3-Benzodioxole – Wikipedia,
Dioxole | C3H4O2 – PubChem

Synthesis of 3-aryl-5-R-thio-[1,3]thiazolo[4′,5′:4,5]pyrimido[1,6-a]benzimidazole-2(3H)-thiones was written by Ivachtchenko, Alexandre;Kovalenko, Sergiy;Parkhomenko, Olexiy;Chernykh, Valentyn. And the article was included in Heterocyclic Communications in 2002.SDS of cas: 4360-63-8 This article mentions the following:

A new five-component condensation of isothiocyanates R¹C₆H₄NCS (R¹ = 4-EtO, 3-MeO), sulfur, 2-(cyanomethyl)benzimidazole, triethylamine and carbon disulfide furnishes triethylammonium 3-aryl-[1,3]thiazolo[4′,5′:4,5]pyrimido[1,6-a]benzimidazole-2(3H)-thioxo-5-thiolates I, the alkylation of which gives 3-aryl-5-R-thio-[1,3]thiazolo[4′,5′:4,5]pyrimido[1,6-a]benzimidazole-2(3H)-thiones II (R² = Me, CH₂CO₂Et, Q). In the experiment, the researchers used many compounds, for example, 2-Bromomethyl-1,3-dioxolane (cas: 4360-63-8SDS of cas: 4360-63-8).

2-Bromomethyl-1,3-dioxolane (cas: 4360-63-8) belongs to dioxole derivatives. Dioxoles, particularly fluorinated dioxoles, are used as co-monomers to make polymers that find use in forming protective coatings for chemical resistance. Dioxole functionalized metal-organic frameworks have also been recently reported.SDS of cas: 4360-63-8

Referemce:
1,3-Benzodioxole – Wikipedia,
Dioxole | C3H4O2 – PubChem

Cascade radical reaction of substrates with a carbon-carbon triple bond as a radical acceptor was written by Miyabe, Hideto;Asada, Ryuta;Takemoto, Yoshiji. And the article was included in Beilstein Journal of Organic Chemistry in 2013.Quality Control of 2-Bromomethyl-1,3-dioxolane This article mentions the following:

The limitation of hydroxamate ester as a chiral Lewis acid coordination moiety was demonstrated in an intermol. reaction involving a radical addition and sequential allylation processes. Next, the effect of hydroxamate ester was studied in the cascade addition-cyclization-trapping reaction of substrates with a carbon-carbon triple bond as a radical acceptor. When substrates with a methacryloyl moiety and a carbon-carbon triple bond as two polarity-different radical acceptors were employed, the cascade reaction proceeded effectively. A high level of enantioselectivity was also obtained by a proper combination of chiral Lewis acid and these substrates. In the experiment, the researchers used many compounds, for example, 2-Bromomethyl-1,3-dioxolane (cas: 4360-63-8Quality Control of 2-Bromomethyl-1,3-dioxolane).

2-Bromomethyl-1,3-dioxolane (cas: 4360-63-8) belongs to dioxole derivatives. Dioxoles, particularly fluorinated dioxoles, are used as co-monomers to make polymers that find use in forming protective coatings for chemical resistance. Dioxole functionalized metal-organic frameworks have also been recently reported.Quality Control of 2-Bromomethyl-1,3-dioxolane

Referemce:
1,3-Benzodioxole – Wikipedia,
Dioxole | C3H4O2 – PubChem

Zn/CuI-Mediated Coupling of Alkyl Halides with Vinyl Sulfones, Vinyl Sulfonates, and Vinyl Sulfonamides was written by Zhao, Matthew M.;Qu, Chuanxing;Lynch, Joseph E.. And the article was included in Journal of Organic Chemistry in 2005.Category: dioxole This article mentions the following:

A novel high-yielding Zn/CuI-mediated coupling of alkyl halides with vinyl sulfones, vinyl sulfonates, and vinyl sulfonamides is described. This protocol is applicable for primary, secondary, and tertiary alkyl iodides and bromides. Alkyl chlorides and aryl and vinyl halides were unreactive under the reaction conditions. Formamide was found to be a superior solvent for obtaining high yields. In the experiment, the researchers used many compounds, for example, 2-Bromomethyl-1,3-dioxolane (cas: 4360-63-8Category: dioxole).

2-Bromomethyl-1,3-dioxolane (cas: 4360-63-8) belongs to dioxole derivatives. Dioxoles, particularly fluorinated dioxoles, are used as co-monomers to make polymers that find use in forming protective coatings for chemical resistance. Dioxole functionalized metal-organic frameworks have also been recently reported.Category: dioxole

Referemce:
1,3-Benzodioxole – Wikipedia,
Dioxole | C3H4O2 – PubChem

1,2,4-Benzothiadiazine derivatives as α₁ and 5-HT_1A receptor ligands was written by Tait, Annalisa;Luppi, Amedeo;Franchini, Silvia;Preziosi, Elisa;Parenti, Carlo;Buccioni, Michela;Marucci, Gabriella;Leonardi, Amedeo;Poggesi, Elena;Brasili, Livio. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2005.Reference of 4360-63-8 This article mentions the following:

A series of 1,2,4-benzothiadiazine derivatives I (R = H, Me, Cl) and II with an arylpiperazine moiety linked at position 3 of the heterocyclic ring were synthesized and assessed for their pharmacol. profiles at α₁-adrenoceptor subtypes (α_1A, α_1B and α_1D) by functional experiments and by in vitro binding studies at human cloned 5-HT_1A receptor. I (R = H) was identified as a α_1D antagonist (pK_bα_1D = 7.59; α_1D/α_1A > 389; α_1D/α_1B = 135) with high selectivity over 5-HT_1A receptor (5-HT_1A/α_1D < 0.01), while II (R = Cl) was characterized as a 5-HT_1A receptor ligand, highly selective over α_1D-adrenoceptor subtype (pK_i5-HT_1A = 8.04; 5-HT_1A/α_1D = 1096). Further pharmacol. studies demonstrated that II (R = Cl) was a partial agonist at 5-HT_1A receptor (E_max = 23, pD₂ = 6.92). In the experiment, the researchers used many compounds, for example, 2-Bromomethyl-1,3-dioxolane (cas: 4360-63-8Reference of 4360-63-8).

2-Bromomethyl-1,3-dioxolane (cas: 4360-63-8) belongs to dioxole derivatives. Dioxoles, particularly fluorinated dioxoles, are used as co-monomers to make polymers that find use in forming protective coatings for chemical resistance. 1,3-Benzodioxole can be synthesized from catechol with disubstituted halomethanes.Reference of 4360-63-8

Referemce:
1,3-Benzodioxole – Wikipedia,
Dioxole | C3H4O2 – PubChem

eCF309: a potent, selective and cell-permeable mTOR inhibitor was written by Fraser, Craig;Carragher, Neil O.;Unciti-Broceta, Asier. And the article was included in MedChemComm in 2016.COA of Formula: C4H7BrO2 This article mentions the following:

Kinase inhibitors capable of blocking the phosphorylation of protein substrates with high selectivity are essential to probe and elucidate the etiol. role of such mols. and their signalling pathways. By addressing these biochem. questions in disease relevant cell-based and in vivo models, strong pharmacol. evidence can be generated towards validating or disproving a target hypothesis. Pharmacol. studies can also provide fundamental information to identify appropriate biomarkers and rational drug combination strategies and thereby facilitate clin. translation. However, due to the high number of kinases encoded by the human genome (>500) and their highly conserved catalytic domains, the development of such an elite class of inhibitors-a.k.a. high-quality chem. probes-represents a major challenge. Through a ligand-based inhibitor design, focused library synthesis and phenotypic screening to prioritize compounds with potent cell activity, we recently identified a cell cycle inhibitor with micromolar potency that inhibits mTOR kinase activity. Following a rapid lead optimization campaign, we report the development of eCF309, an mTOR inhibitor displaying low nanomolar potency both in vitro and in cells and an excellent selectivity profile (S-score (35%) = 0.01 at 10 μM). In the experiment, the researchers used many compounds, for example, 2-Bromomethyl-1,3-dioxolane (cas: 4360-63-8COA of Formula: C4H7BrO2).

2-Bromomethyl-1,3-dioxolane (cas: 4360-63-8) belongs to dioxole derivatives. Dioxoles, particularly fluorinated dioxoles, are used as co-monomers to make polymers that find use in forming protective coatings for chemical resistance. 1,3-Benzodioxole can be synthesized from catechol with disubstituted halomethanes.COA of Formula: C4H7BrO2

Referemce:
1,3-Benzodioxole – Wikipedia,
Dioxole | C3H4O2 – PubChem