Catalyst‐Free Protocol for the Synthesis of Quinoxalines and Pyrazines in PEG

A facile and simple catalyst‐free protocol has been developed for the condensation of 1,2‐diketones with aromatic 1,2‐diamines in polyethylene glycol (PEG), providing quinoxaline derivatives in good yields. The important features of the methodology are broad substrates scope, simple workup, catalyst free, environmentally benign, and no requirement for metal catalysts. It is noteworthy that the cyclization reaction of 1,2‐diketones with aliphatic 1,2‐diamines is also conducted smoothly to afford pyrazines in good yields under the standard conditions. In addition, PEG could be recovered easily and was reused without evident loss in activity     

Preparation and evaluation of <Superscript>131</Superscript>I-quercetin as a novel radiotherapy agent against dedifferentiated thyroid cancer

Here we reported the radiolabeling and evaluation of a novel ¹³¹I-radiolabeled quercetin for the treatment of dedifferentiated thyroid cancers. The human thyroid cancer cell lines (FTC-133, TT and DRO) experienced much higher uptake of ¹³¹I-quercetin as compared to the free ¹³¹I. And the proliferation inhibition rate of ¹³¹I-quercetin on in vitro DRO cell line was 86.87 ± 7.15%. Biodistribution and SPECT analysis demonstrated that the injected radioactivity mainly accumulated in tumors. The tumor volume in the treatment group was dramatically inhibited in comparison with the control group.     

Camptothecin@HMSNs/thermosensitive hydrogel composite for applications in preventing local breast cancer recurrence

The CPT was loaded into the HMSNs with the high loading capacity. Then the CPT@HMSNs were loaded into the PLEL thermosensitive hydrogels for local therapy to prevent the recurrence of breast cancer after the tumor was resected.     

Well‐controlled ring‐opening polymerization of cyclic esters catalyzed by aluminum amido complexes: Kinetics and mechanism

A series of aluminum dimethyl complexes 1 – 6 bearing N‐[2‐(pyrrolidinyl)benzyl]anilido ligands were synthesized and well characterized. The molecular structure of complex 1 determined by an X‐ray diffraction study indicates the bidentate chelating mode of the pyrrolidinyl‐anilido ligand. In the absence of a coinitiator, these complexes exhibited excellent control toward the polymerizations of ε‐caprolactone and rac‐lactide, affording polyesters with quite narrow molecular weight distributions (M_w/M_n = 1.04–1.26). The end group analysis of ε?CL oligomer via ¹H NMR and ESI‐TOF MS methods gave strong support to the hypothesis that the polymerization catalyzed by these aluminum complexes proceeds via a coordination‐insertion mechanism involving a unique Al? N (amido) bond initiation. Via ¹H NMR scale oligomerization studies, it is suggested that the insertion of the first lactide monomer into Al? N bond of the complex is much easier than the insertion of lactide monomer into the newly formed Al? O (lactate) bond and might also be easier than the insertion of the first ε?CL monomer into Al? N bond. © 2014 Wiley Periodicals, Inc. J. Polym. Sci., Part A: Polym. Chem. 2014 , 52, 3096–3106