Guolin Zhang

Publications (5)14.27 Total impact

• Article: Synthesis and antitumor evaluation of a novel class of 4-substituted-1,4-dihydroisoquinolin-3-ones.

  Ting Ma, Wenteng Chen, Guolin Zhang, Yongping Yu
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  ABSTRACT: An efficient method for the solution-phase parallel synthesis of 4-substituted-1,4-dihydroisoquinolin-3-ones is developed. The isoquinolinones were constructed employing an intramolecular Heck reaction, providing full regio- and stereoselectivity. Most of the synthesized compounds showed potent antiproliferative activities against tumor cell lines.
  Journal of Combinatorial Chemistry 07/2010; 12(4):488-90. · 3.41 Impact Factor
• Article: Traceless Approach for the Synthesis of 3,5-Disubstituted Thiohydantoins on Functionalized Ionic-Liquid Support

  Chao Yao, Yandong Zhang, Guolin Zhang, Wenteng Chen, Yongping Yu, Richard A. Houghten
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  ABSTRACT: A traceless approach for the synthesis of 3,5-disubstituted thiohydantoins on a novel functionalized ionic-liquid support, 5, is described. Acylation of benzylamine functionalized ionic-liquid support with amino acids yielded ionic-liquid-supported amino acids, which reacted with isothiocyanates to afford ionic-liquid-supported thioureas. Following intramolecular cyclization cleavage from the ionic-liquid support by trifluoroacetic acid (TFA), the desired 3,5-disubstituted thiohydantoins were obtained in good yields and purities. The efficiency of this ionic-liquid-phase strategy facilitated isolation and analysis of intermediates and removal of excess reagents and by-products during the reaction process.
  Synthetic Communications - SYN COMMUN. 01/2010; 40(5):717-724.
• Article: Synthesis and antitumor activities of 2‐(substituted)phenyl‐1,2,4‐triazolo[1,5‐a]pyridines

  Guolin Zhang, Yongzhou Hu
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  ABSTRACT: Twenty-three 2-(substituted)phenyl-1,2,4-triazolo[1,5-a]pyridines have been synthesized by cycloadditison reaction between N-amino methylpyridinium mesitylenesulfonates and substituted benzonitriles under the presence of potassium hydroxide at room temperature. The structures of all products were confirmed by 1H NMR, MS and elemental analyses. The antitumor activities of these compounds were evaluated against human ovary cancer cell line (HO-8910) in vitro by MTT method. The preliminary results showed that compound 1e (IC50 28μM) and compound 1w (IC50 31μM) exhibited stronger antitumor activities than cisplatin (IC50 35μM) in vitro. Hence, 1e and 1w have potential antitumor activities and are worth further investigation.
  Journal of Heterocyclic Chemistry 03/2009; 44(4):919 - 922. · 1.22 Impact Factor
• Article: Solid-phase synthesis and antitumor evaluation of 2,4-diamino-6-aryl-1,3,5-triazines.

  Zhang Hu, Ting Ma, Zhe Chen, Ziqi Ye, Guolin Zhang, Yijia Lou, Yongping Yu
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  ABSTRACT: 2,4-Diamino-6-aryl-1,3,5-triazines were synthesized by using a solid-supported approach in which monoarylsubstituted triazines were captured directly from the crude reaction mixture by resin-bound amines. The effects of the synthesized compounds on inhibition activities against tumor cell lines (PC-3, K562, A549, and HO8910) were examined. Most of the obtained compounds demonstrated remarkable antiproliferative activities against K562, PC-3, and HO8910 cell lines. Particularly, compounds 8c exhibited prominent inhibition activity with IC(50) values of 1.01, 2.23, and 1.06 microM, respectively. The structure-activity relationships of 2,4-diamino-6-aryl-1,3,5-triazines are also discussed.
  Journal of Combinatorial Chemistry 02/2009; 11(2):267-73. · 3.41 Impact Factor
• Article: An efficient one-pot synthesis of 5, 9-cyclo-1, 11-oxido-pregn-16-ene-3, 20-dione from 9-bromide-11-hydroxypregna-1, 4, 16-trien-3, 20-dione by two annulation reactions.

  Ping Jia, Xuling Wu, Yongping Yu, Guolin Zhang
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  ABSTRACT: An efficient method to prepare 5, 9-cyclo-1, 11-oxido-pregn-16-ene-3, 20-dione in one pot was reported. Treatment of 9-bromide-11-hydroxypregna-1, 4, 16-trien-3, 20-dione with Raney Ni in absolute ethanol afforded 5, 9-cyclo-1, 11-oxido-pregn-16-ene-3, 20-dione by two annulation reactions in reasonable yield. The absolute configuration was also confirmed by X-ray crystal analysis.
  Steroids 12/2008; 74(2):229-32. · 2.83 Impact Factor
• Article: A traceless approach for the solid-phase parallel synthesis of trisubstituted oxindoles.

  Jinwen Xie, Jing Sun, Guolin Zhang, Richard A Houghten, Yongping Yu
  Journal of Combinatorial Chemistry 9(4):566-8. · 3.41 Impact Factor