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161.
Mian Fu Xiaomei Zhuang Tianhong Zhang Ying Guan Qingbin Meng Yongjun Zhang 《Macromolecular bioscience》2020,20(9)
Leuprolide has been widely used in androgen deprivation therapy for the treatment of advanced prostate cancer, but its use is still limited due to its short half‐life. Herein, hydrogen‐bonded layer‐by‐layer films are fabricated from PEGylated leuprolide (PEG‐LEU) and tannic acid (TA). Because of its dynamic nature, the film disintegrates gradually in water and releases PEG‐LEU and TA. The in vitro release profile indicated perfect zero‐order kinetics, which is explained by the unique release mechanism. When implanted subcutaneously in male rats, the films maintain a constant serum drug level. For a 60‐bilayer film, the serum drug level is maintained constant for ≈24 days. No initial burst release is observed, suggesting that the in vivo release also follows zero‐order kinetics. Initially, an increase in the level of serum testosterone is induced by the released drug, followed by testosterone suppression to a constant level below the castrate level, which could be maintained as long as a constant serum drug level is maintained. Since the new drug carriers avoid an initial burst release of the drug and maintain a constant serum drug level and hence a constant serum testosterone level below the castrate level, these carriers are highly promising for androgen deprivation therapy. 相似文献
162.
Metal‐Free Reaction of ortho‐Carbonylated Alkynyl‐Substituted Arylaldehydes with Common Amines: Selective Access to Functionalized Isoindolinone and Indenamine Derivatives 下载免费PDF全文
Dr. Ziping Cao Hongbo Zhu Dr. Xin Meng Jun Guan Qiang Zhang Laijin Tian Xuejun Sun Guang Chen Prof. Dr. Jinmao You 《Chemistry (Weinheim an der Bergstrasse, Germany)》2016,22(47):16979-16985
Herein we describe a reaction of ortho‐carbonylated alkynyl‐substituted arylaldehydes with common primary amines that can provide functionalized isoindolinone and 3‐hydroxylindenamine products in high yields. Depending on the substituent size of primary amines, two distinct reaction pathways were exploited selectively, that are, an initial aza‐conjugate addition followed by hydrogen transfer to access isoindolinone framework and a unique oxa‐conjugate addition followed by Petasis–Ferrier rearrangement to afford indenamine derivatives. In the presence of Et3N, the reaction property of small primary amines was changed, proceeding to afford 3‐hydroxylindenamine derivatives efficiently. These products contain interesting substructures that exist in many natural products and bioactive molecules. The reaction features contain the use of transition‐metal‐free catalysts, simple operation, broad substrate scope, and product diversity. 相似文献
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Herein we discovered that a Nile Red-based probe with a cinnamoyl unit was highly selective and sensitive to N2H4. Hydrazinolysis by N2H4 would release a hydroxyl substituted Nile Red and result in remarkable fluorescence quench. Importantly, Cys/Hcy would not interrupt the N2H4 recognition. This is because, for this probe, the combination of the π-π conjugate system can stabilize the ethylene union, which results in the nucleophilic addition of the thiol group of Cys/Hcy becomes non-effective. 相似文献
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An efficient strategy enabling the construction of polysubstituted 1,2-dihydroquinoline derivatives mediated by the commercially available, economical, and environmentally benign iodine (3 mol %) under mild conditions was developed. Various arylamines and α-ketoesters could participate in this cascade reaction, and the desired products were obtained in excellent yields up to 98%. 相似文献
167.
An efficient one‐pot method for the synthesis of hydroxyflavanones is described. Methoxychalcones are treated with 36% HBr to afford cyclization and regioselective O‐demethylation products (2a–i) while cyclization and complete O‐demethylation products (3a–e) are obtained in the presence of 45% HI. 相似文献
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Dr. Zhen Lei Zong‐Jie Guan Dr. Xiao‐Li Pei Shang‐Fu Yuan Xian‐Kai Wan Jin‐Yuan Zhang Prof.Dr. Quan‐Ming Wang 《Chemistry (Weinheim an der Bergstrasse, Germany)》2016,22(32):11156-11160
A red–near‐IR dual‐emissive nanocluster with the composition [Au10Ag2(2‐py?C≡C)3(dppy)6](BF4)5 ( 1 ; 2‐py?C≡C is 2‐pyridylethynyl, dppy=2‐pyridyldiphenylphosphine) has been synthesized. Single‐crystal X‐ray structural analysis reveals that 1 has a trigonal bipyramidal Au10Ag2 core that contains a planar Au4(2‐py?C≡C)3 unit sandwiched by two Au3Ag(dppy)3 motifs. Cluster 1 shows intense red–NIR dual emission in solution. The visible emission originates from metal‐to‐ligand charge transfer (MLCT) from silver atoms to phosphine ligands in the Au3Ag(dppy)3 motifs, and the intense NIR emission is associated with the participation of 2‐pyridylethynyl in the frontier orbitals of the cluster, which is confirmed by a time‐dependent density functional theory (TD‐DFT) calculation. 相似文献