Yan Li

Publications (2)6.19 Total impact

• Article: Synthesis and antitumor activity of novel dithiocarbamate substituted chromones.

  Wei Huang, Yu Ding, Yan Miao, Ming-Zhen Liu, Yan Li, Guang-Fu Yang
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  ABSTRACT: A series of chromone derivatives bearing diverse dithiocarbamate moieties were designed and synthesized via a three-component reaction protocol. Their in vitro antitumor activities were evaluated by MTT method against HCCLM-7, Hela, MDA-MB-435S, SW-480, Hep-2 and MCF-7. Two compounds (3-chloro-4-oxo-4H-chromen-2-yl)methyl piperidine-1-carbodithioate (Iq) and (6-chloro-4-oxo-4H-chromen-3-yl)methyl piperidine-1-carbodithioate (IIu), were identified as the most promising candidate due to their high potency and broad-spectrum. Further flow-activated cell sorting analysis revealed that compounds Iq and IIu arrest the cell cycle of SW-480 and MDA-MB-435s both in G(2)/M phase with dose-dependent effect and might display apoptosis-inducing effect on these tumor cell lines.
  European journal of medicinal chemistry 05/2009; 44(9):3687-96. · 3.27 Impact Factor
• Article: Design, syntheses, and antitumor activity of novel chromone and aurone derivatives.

  Wei Huang, Ming-Zhen Liu, Yan Li, Ying Tan, Guang-Fu Yang
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  ABSTRACT: A series of new chromone analogues bearing heterocyclic thioether moiety and aurone analogues bearing cyclic tertiary amine moiety were designed and synthesized under microwave irradiation. The synthetic protocol was found to present many advantages, such as higher yields, shorter reaction time (10-20 min), mild condition, and readily isolation of the products. The synthesized compounds were assayed for their antitumor activity against four kinds of human solid tumor cell lines including HCCLM-7, Hep-2, MDA-MB-435S, and SW-480. Two compounds, (Z)-2-((4-benzyl-piperazin-1-yl)methylene)benzofuran-3(2H)-one 5e and (Z)-2-((4-(bis(4-fluorophenyl)methyl)piperazin-1-yl)methylene)benzofuran-3(2H)-one 5f, were identified as the most promising candidates with the IC(50) values in the range of 4.1-13.1 microM. Further cell cycle studies revealed that compounds 5e and 5f arrest the cell cycle in G(0)/G(1) phase and displayed apoptosis-inducing effect on Hep-2 cells.
  Bioorganic & Medicinal Chemistry 09/2007; 15(15):5191-7. · 2.92 Impact Factor