Hai-Xia Jiang

Shanghai Research Institute of Chemical Industry, Shanghai, Shanghai Shi, China

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Publications (5)13.71 Total impact

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    ABSTRACT: A novel series of trifluoromethyl indole derivatives have been designed, synthesized and evaluated for anti-HIV-1 activities in MT-2 cells. The hydrophobic constant, acute toxicity, carcinogenicity and mutagenicity were predicted. Trifluoromethyl indoles and showed extremely promising activities against WT HIV-1 with IC50 values at the low nanomolar level, similar to efavirenz, better than nevirapine, and also possessed higher potency towards the drug-resistant mutant strain Y181C than nevirapine. Preliminary SAR and docking studies of detailed binding mode provided some insights for discovery of more potent NNRTIs.
    Organic & Biomolecular Chemistry 04/2014; 12(21). DOI:10.1039/c3ob42186d · 3.56 Impact Factor
  • Yan-Jun Chen · Hai-Xia Jiang · Kun Gao
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    ABSTRACT: Phytochemical investigation of Eupatorium fortunei Turcz. afforded one novel 30-nor-ursane triterpene, 3β-hydroxy-30-nor-urs-21-en-20-one, and seven known compounds including two sesquiterpenes and five monoterpenes. These eight compounds were isolated from the genus Eupatorium for the first time. These finds may be chemotaxonomically significant to distinguish E. fortunei from other Eupatorium species.
    Biochemical Systematics and Ecology 04/2013; 47:1–4. DOI:10.1016/j.bse.2012.10.008 · 0.97 Impact Factor
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    ABSTRACT: Compound 1 ((-)-gossypol) has been long known as a chemical anticancer agent. With its low water solubility and toxicity, it is not widely used as a commercial drug. To overcome these disadvantages, several novel derivatives of gossypol were designed, synthesized, and analyzed. One of the derivatives, compound 7 (6-aminopenicillanic acid sodium-gossypolone), was identified with great water solubility and anticancer property, suggested by inducing a dramatically decrease in Bcl-2 and Bcl-xL protein expression level found in vitro and growth inhibition of murine colon tumor in vivo. Furthermore, it was also recognized with less toxicity than compound 1 in vivo and significantly increased chemotherapeutic sensitivity against colon cancer in combination with traditional chemotherapeutic agent 5-fluorouracil. Therefore, it is concluded that compound 7 is superior to parent compound 1, and further preclinical studies of compound 7 is necessary for colon cancer therapy.
    Journal of Medicinal Chemistry 08/2010; 53(15):5502-10. DOI:10.1021/jm1001698 · 5.45 Impact Factor
  • Hai-Xia Jiang · Xing-Xin Cao · Hao Huang · Biao Jiang
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    ABSTRACT: A simple and practical procedure has been developed for the resolution of racemic gossypol. The commercially available l-amino acid esters have been employed as the resolving agents with the l-tryptophan methyl ester (l-Trp-OMe) as the best reagent of choice. The individual diastereoisomeric gossypol adducts derived from l-Trp-OMe are readily separated by a simple filtration step to give the (−)-diastereoisomeric adduct, and its (+)-diastereoisomeric adduct can be easily obtained by simple evaporation of the mother liquor. Acid hydrolysis of the separated adduct gave (−)-gossypol and (+)-gossypol, respectively, in high chemical yields (quantitatively) and in high enantiomeric excesses (>95%).
    Tetrahedron Asymmetry 10/2007; 18(20):2437-2441. DOI:10.1016/j.tetasy.2007.09.032 · 2.16 Impact Factor
  • Source
    Xin Zhao · Hai-Xia Jiang · Hao Huang · Rui-Liang Zhu · Biao Jiang
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    ABSTRACT: A new bidihydroflavonoid, thuidinin 1, together with 5 known compounds including one known biflavonoid 3′,3′′′-binaringenin (2) and four other known natural products pentadecane (3), methyl β-orcinolarboxylate (4), β-sitosterol (5) and daucostenol (6), were isolated from leaves of Thuidium kanedae Sak. Their structures were established on the basis of 1D and 2D spectroscopic analysis. The absolute stereochemistry of compounds 1 and 2 was determined by CD spectra.
    Chinese Journal of Chemistry 03/2006; 24(3):393 - 395. DOI:10.1002/cjoc.200690075 · 1.58 Impact Factor