Category: 211315-53-6

Hu, Quan-Fang published the artcileDesign, synthesis and biological evaluation of novel 1-phenyl phenanthridin-6(5H)-one derivatives as anti-tumor agents targeting TOPK, Synthetic Route of 211315-53-6, the main research area is OTS964 phenanthridin synthesis antitumor apoptosis TOPK colorectal cancer; 1-Phenyl phenanthridin-6(5H)-one; Colorectal cancer; Pharmacokinetics; Structure activity relationship; TOPK inhibitor.

T-lymphokine-activated killer cell-originated protein kinase (TOPK) is a serine-threonine mitogen-activated protein kinase that is highly expressed in many types of human cancer. Due to its important role in cancer progression, TOPK is becoming an attractive target in chemotherapeutic drug design. In this study, a series of 1-Ph phenanthridin-6(5H)-one derivatives have been identified as a novel chem. class of TOPK inhibitors. Some of them displayed very potent anti-cancer activity with IC50s less than 100 nM, superior than reference compound OTS964. The most potent compound, 9g suppressed the growth of cancer cells by apoptosis and specifically inhibited the activities of TOPK. Oral administration of 9g effectively suppressed tumor growth with TGI >79.7% in colorectal cancer xenograft models, demonstrating superior efficacy compared to OTS964. Pharmacokinetic studies reveal its good oral bioavailability. Our findings therefore show that 9g is a specific inhibitor of TOPK both in vitro and in vivo that may be further developed as a potential therapeutic agent against colorectal cancer.

European Journal of Medicinal Chemistry published new progress about Antitumor agents. 211315-53-6 belongs to class bromides-buliding-blocks, name is (R)-tert-Butyl (2-(4-bromophenyl)propyl)carbamate, and the molecular formula is C14H20BrNO2, Synthetic Route of 211315-53-6.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Cabre, Albert published the artcileHighly Enantioselective Iridium-Catalyzed Hydrogenation of 2-Aryl Allyl Phthalimides, Recommanded Product: (R)-tert-Butyl (2-(4-bromophenyl)propyl)carbamate, the main research area is beta aryl methyl amine preparation enantioselective; aryl allyl phthalimide hydrogenation iridium catalyst.

The iridium-catalyzed asym. hydrogenation of 2-aryl allyl phthalimides to afford enantioenriched β-aryl-β-Me amines is presented. Recently developed Ir-MaxPHOX catalysts are used for this enantioselective transformation. The mild reaction conditions and the feasible removal of the phthalimido group makes this catalytic method easily scalable and of great interest to afford chiral amines. The importance of this new methodol. is exemplified by the formal synthesis of (R)-Lorcaserin, OTS514, and enantiomerically enriched 3-Me indolines.

Organic Letters published new progress about Amines Role: SPN (Synthetic Preparation), PREP (Preparation). 211315-53-6 belongs to class bromides-buliding-blocks, name is (R)-tert-Butyl (2-(4-bromophenyl)propyl)carbamate, and the molecular formula is C14H20BrNO2, Recommanded Product: (R)-tert-Butyl (2-(4-bromophenyl)propyl)carbamate.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Hebeisen, Paul published the artcileRing opening of cyclic sulfamidates with bromophenyl metal reagents: complementarity of sulfamidates and aziridines, Related Products of bromides-buliding-blocks, the main research area is cyclic sulfamidate preparation aryl iodide derived Grignard ring opening; stereochem inversion regioselective ring opening.

Bromophenyl magnesium reagents generated via a Knochel type magnesium-halogen exchange of aryl iodides undergo regioselective ring opening of cyclic primary and secondary N-Boc sulfamidates in good to excellent yields. With secondary sulfamidates the reaction proceeds with clean inversion of the stereochem. This protocol complements the ring opening of aziridines with bromophenyl metal reagents and extends its scope to secondary substrates.

Tetrahedron Letters published new progress about Amino alcohols Role: RCT (Reactant), RACT (Reactant or Reagent). 211315-53-6 belongs to class bromides-buliding-blocks, name is (R)-tert-Butyl (2-(4-bromophenyl)propyl)carbamate, and the molecular formula is C14H20BrNO2, Related Products of bromides-buliding-blocks.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary