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        Synthesis and Cytotoxicity Evaluation of New 3-substituted 4-(4-methyloxy phenyl)-1H-Pyrrole Derivatives

        Xiaoping Zhan,Lan Lan,Yuankui Zhang,Jian Chen,Kai Zhao,Shuai Wang,Yuxuan Xin,Zhenmin Mao 대한화학회 2016 Bulletin of the Korean Chemical Society Vol.37 No.2

        A new series of 3-substituted 4-(4-methyloxy phenyl)-1H-pyrrole derivatives were synthesized and biologically evaluated for potential anticancer activity. Fifteen targeted compounds showed high selectivity toward normal cells and cancer cells: that is, all targeted compounds had no obvious cytotoxicity toward normal human cells (HUVEC and NIH/3T3), but some compounds exhibited broad-spectrum proliferation inhibitory activity against the screened cancer cell lines. Among these pyrrole derivatives, compounds 3b and 3o showed potent anticancer activity against the MG-63 cell line, with IC50 values of 14.9 and 12.7 μM, respectively. Other pyrrole derivatives also showed promising proliferation inhibitory activity, including compound 3d against A375 (IC50 = 18.6 μM), compound 3f and 3j against MGC80-3 (IC50 = 19.9 μM), and compound 3o against MGC80-3 (IC50 = 11.9 μM). Because the developed pyrrole derivatives showed strong anticancer activity and high selectivity, this new series of pyrrole derivatives could be considered as promising lead compounds for further development of potent and safe anticancer agents.

      • Cyclo[<i>m</i>]pyridine[<i>n</i>]pyrroles: Hybrid Macrocycles That DisplayExpanded π-Conjugationupon Protonation

        Zhang, Zhan,Lim, Jong Min,Ishida, Masatoshi,Roznyatovskiy, VladimirV.,Lynch, Vincent M.,Gong, Han-Yuan,Yang, Xiaoping,Kim, Dongho,Sessler, Jonathan L. American Chemical Society 2012 JOURNAL OF THE AMERICAN CHEMICAL SOCIETY - Vol.134 No.9

        <P>Novel hybrid cyclo[<I>m</I>]pyridine[<I>n</I>]pyrroles have been synthesized using Suzuki coupling.Their NMRand optical spectroscopic features and solid state structural parametersprovide support for the proposal that these species are best describedas locally aromatic compounds devoid of long-range intersubunit conjugation.However, an extension of the π-conjugation in the macrocyclescan be realized through protonation, as inferred from optical spectroscopicand X-ray diffraction-based structural studies.</P><P><B>Graphic Abstract</B> <IMG SRC='http://pubs.acs.org/appl/literatum/publisher/achs/journals/content/jacsat/2012/jacsat.2012.134.issue-9/ja211985k/production/images/medium/ja-2011-11985k_0006.gif'></P><P><A href='http://pubs.acs.org/doi/suppl/10.1021/ja211985k'>ACS Electronic Supporting Info</A></P>

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        Urinary Hypoxia-Inducible Factor-1alpha Levels Are Associated with Histologic Chronicity Changes and Renal Function in Patients with Lupus Nephritis

        Chunyang Ma,Zhuori Li,Jiali Wei,Feng Zhan,Ru Wang,Keying Fu,Xiaoping Wan 연세대학교의과대학 2012 Yonsei medical journal Vol.53 No.3

        Purpose: Tubulointerstitial hypoxia in the kidney is considered a hallmark of injury and a mediator of the progression of tubulointerstitial fibrosis. Hypoxia-inducible factor-1alpha (HIF-1alpha), a master transcription factor in cellular adaptation to hypoxia,regulates a wide variety of genes, some of which are closely associated with tissue fibrosis. The present study set out to characterize urinary HIF-1alpha expressions in patients with lupus nephritis (LN) and to explore whether urinary HIF-1alpha expressions are associated with histologic chronicity changes and renal function. Materials and Methods: Urinary HIF-1alpha levels were measured by enzyme-linked immunosorbent assays in 42 patients with LN and in 30 healthy controls. Activity and chronicity indexes as well as tubular HIF-1alpha expressions were analyzed for each specimen. Results: Urinary HIF-1alpha levels were higher in LN patients than in healthy controls (3.977±1.696 vs. 2.153±0.554 ng/mL, p<0.001) and were associated with histologic chronicity indexes (r=0.463, p<0.01) and eGFR (r=-0.324, p<0.05). However, urinary HIF-1alpha levels showed no correlation with histologic activity indexes, anti-dsDNA, ANA, complement 3 and 4 levels, proteinuria, systemic lupus erythematosis disease activity index, and WHO pathological classification (p>0.05). Conclusion: Urinary HIF-1alpha levels were elevated in LN patients and were associated with histologic chronicity changes and renal function, indicating that HIF-1alpha might contribute to histologic chronicity in LN.

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