854778-30-6 Archives - Chlorides-buliding-blocks

Liu, Jing-Jing’s team published research in ChemMedChem in 16 | CAS: 854778-30-6

ChemMedChem published new progress about 854778-30-6. 854778-30-6 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Boronic acid and ester,Benzene,Ether,Boronic Acids,Boronic acid and ester, name is (2-Chloro-3-methoxyphenyl)boronic acid, and the molecular formula is C7H8BClO3, Category: chlorides-buliding-blocks.

Liu, Jing-Jing published the artcileDiscovery of Antimetastatic Chiral Ionone Alkaloid Derivatives Targeting HIF-1α/VEGF/VEGFR2 Pathway, Category: chlorides-buliding-blocks, the publication is ChemMedChem (2021), 16(13), 2130-2145, database is CAplus and MEDLINE.

Novel chiral ionone alkaloid derivatives were synthesized and their antimetastatic effects were evaluated in human breast cancer cells using chemotaxis assay. Compared with pos. control LY294002, a PI3 K inhibitor, seven derivatives exhibited significant inhibitory effects against cancer cell migration. Especially, the IC₅₀ for compound I was as low as 0.035±0.004μM. Further investigations on compound I revealed that it could exert inhibitory effects on the adhesion, migration and invasion of MDA-MB-231 cells. The mechanisms for the antitumor metastatic effects of I might be through the inhibition of HIF-1α/VEGF/VEGFR2/Akt pathway, which suppressed the downstream signaling mols., including Akt1/mTOR/p70S6K and Akt2/PKCζ/integrin β1 pathways. Taken together, chiral ionone alkaloid derivative I has the potential to be developed into an antitumor metastatic agent for breast cancer.

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

Fang, Chao’s team published research in Bioorganic & Medicinal Chemistry Letters in 28 | CAS: 854778-30-6

Bioorganic & Medicinal Chemistry Letters published new progress about 854778-30-6. 854778-30-6 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Boronic acid and ester,Benzene,Ether,Boronic Acids,Boronic acid and ester, name is (2-Chloro-3-methoxyphenyl)boronic acid, and the molecular formula is C7H8BClO3, Computed Properties of 854778-30-6.

Fang, Chao published the artcileDiscovery of heterocyclic replacements for the coumarin core of anti-tubercular FadD32 inhibitors, Computed Properties of 854778-30-6, the publication is Bioorganic & Medicinal Chemistry Letters (2018), 28(22), 3529-3533, database is CAplus and MEDLINE.

Previous work established a coumarin scaffold as a starting point for inhibition of Mycobacterium tuberculosis (Mtb) FadD32 enzymic activity. After further profiling of the coumarin inhibitor 4 revealed chem. instability, the authors discovered that a quinoline ring circumvented this instability and had the advantage of offering addnl. substitution vectors to further optimize. Ensuing SAR studies gave rise to quinoline-2-carboxamides with potent antitubercular activity. Further optimization of ADME/PK properties culminated in I that exhibited compelling in vivo efficacy in a mouse model of Mtb infection.

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

Pontillo, Joseph’s team published research in Bioorganic & Medicinal Chemistry Letters in 15 | CAS: 854778-30-6

Pontillo, Joseph published the artcileSynthesis of aryl-1,2,4-triazine-3,5-diones as antagonists of the gonadotropin-releasing hormone receptor, Computed Properties of 854778-30-6, the publication is Bioorganic & Medicinal Chemistry Letters (2005), 15(19), 4363-4366, database is CAplus and MEDLINE.

Several efficient synthetic routes for 2-, 4-, and 6-aryl-1,2,4-triazine-3,5-diones were developed. Derivatives were synthesized and studied as gonadotropin-releasing hormone antagonists in an effort to understand structure-activity relationships of the monocyclic compounds One compound was identified as potent gonadotropin-releasing hormone receptor antagonist from this series.

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

Zhao, Liren’s team published research in Bioorganic & Medicinal Chemistry Letters in 18 | CAS: 854778-30-6

Zhao, Liren published the artcile5-Aryluracils as potent GnRH antagonists – Characterization of atropisomers, Related Products of chlorides-buliding-blocks, the publication is Bioorganic & Medicinal Chemistry Letters (2008), 18(11), 3344-3349, database is CAplus and MEDLINE.

Optimization of a series of uracils bearing a 2-fluoro- or 2-chloro-3-methoxyphenyl group at the 5-position resulted in compounds such as I (R = Me, X = CF₃, Y = F, Cl) with subnanomolar binding affinity at the human GnRH receptor. While the 2-fluoro-3-methoxyphenyl compound I (R = X = Y = Me) was characterized as a mixture of interchangeable atropisomers, the diastereoisomers of 2-chloro-3-methoxyphenyl analogs were separated It was found that the aR-atropisomer was much more potent than the aS-isomer based on the X-ray crystal structure of I (R = CH₂OH, X = CF₃, Y = Cl).

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

Guo, Zhiqiang’s team published research in Bioorganic & Medicinal Chemistry Letters in 15 | CAS: 854778-30-6

Guo, Zhiqiang published the artcileUracils as potent antagonists of the human gonadotropin-releasing hormone receptor without atropisomers, SDS of cas: 854778-30-6, the publication is Bioorganic & Medicinal Chemistry Letters (2005), 15(10), 2519-2522, database is CAplus and MEDLINE.

Uracil derivatives I [X¹ = F, CF₃; X² = F, SO₂Me, Cl, MeS, etc.; Y = 2-F-3-OMe, 2-Cl, H, 2-F, etc.] were designed and synthesized to avoid atropisomers observed in the 6-methyluracils as antagonists of the human GnRH receptor. Optimization at the 1- and 5-positions of the uracil resulted in potent compounds such as I [X¹ = F, X² = CF₃, Y = 2-Cl-3-OMe] (K_i = 0.45 nM).

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