108289-24-3Relevant academic research and scientific papers
Convenient Assembly of Privileged (Hetero)Arene-Fused Benzo[1.4]oxazepines via Two Tandem SNAr Events. Part 1 – On the Importance of the Intermittent Smiles Rearrangement
Sapegin, Alexander,Krasavin, Mikhail
, p. 5234 - 5241 (2019/05/08)
New bis-nucleophilic precursors to [1.4]oxazepines synthesized via SNAr-Smiles rearrangement-SNAr cascade have been designed. Employing them in base-promoted condensation with aromatic bis-electrophiles allowed differentiating between highly and poorly reactive substrates (i.e. those which can and cannot pass through the Smiles rearrangement barrier, respectively). The reactivity toward the desired course of cyclization can be restored by introducing electron-withdrawing substituents in the bis-electrophile precursor. This strongly argues for the importance of the Smiles rearrangement for the successful overall ring formation.
Design and synthesis of neolamellarin a derivatives targeting heat shock protein 90
Jiang, Long,Yin, Ruijuan,Wang, Xueting,Dai, Jiajia,Li, Jing,Jiang, Tao,Yu, Rilei
, p. 24 - 33 (2017/04/21)
In this study, we designed and synthesized a novel family of neolamellarin A derivatives that showed high inhibitory activity toward heat shock protein 90 (Hsp90), a kinase associated with cell proliferation. The 3,4-bis(catechol)pyrrole scaffold and the benzyl group with methoxy modification at N position of pyrrole are essential to the Hsp90 inhibitory activity and cytotoxicity of these compounds. Western blot analysis demonstrated that these compounds induced dramatic depletion of the examined client proteins of Hsp90, and accelerated cancer cell apoptosis. Docking simulations suggested that the binding mode of 9p was similar to that of the VER49009, a potent inhibitor of Hsp90. Further molecular dynamics simulation indicated that the hydrophobic interactions as well as the hydrogen bonds contributed to the high affinity of 9p to Hsp90.
Purinenucleoside derivative modified in 8-position and medical use thereof
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Page/Page column 27, (2010/11/28)
The present invention provides an 8-modified purinenucleoside derivative which is useful for diseases associated with an abnormality of plasma uric acid level. An 8-modified purinenucleoside derivative represented by the following formula (I), a prodrug thereof or a pharmaceutically acceptable salt thereof, or a hydrate or solvate thereof, is useful for the prevention or treatment of gout, hyperuricemia, urinary lithiasis, hyperuricemic nephropathy or the like. In the formula, n is 1 or 2; RA is a hydrogen atom or a hydroxyl group; R1 is a hydrogen atom, a hydroxyl group, a thiol group, an amino group or a chlorine atom; ring J represents an optionally substituted 2-naphthyl group, or a group represented by the following general formula (II) wherein Y represents a single bond or a connecting group; ring Z represents an optionally substituted aryl group or heteroaryl group or the like; and R2 to R4, P1 and Q represents a halogen atom, a cyano group or the like.
