Shaohua Gou


Affiliation: Southeast University
Country: China


  1. Chen H, Chen F, Wang X, Gou S. Multifunctional Pt(iv) complexes containing a glutathione S-transferase inhibitor lead to enhancing anticancer activity and preventing metastasis of osteosarcoma cells. Metallomics. 2019;11:317-326 pubmed publisher
    ..Meanwhile, it can prevent the metastasis of OS via down-regulating Akt. Thus, complex 2 has the potential for further research for the treatment of OS. ..
  2. Xu Z, Zhao J, Gou S, Xu G. Novel hypoxia-targeting Pt(iv) prodrugs. Chem Commun (Camb). 2017;53:3749-3752 pubmed publisher
    ..The resulting Pt(iv) prodrug exhibited effective inhibition on tumor growth in the HCT-116 xenograft mouse model with low toxicity in vivo. ..
  3. Sun C, Fang L, Zhang X, Gao P, Gou S. Novel 7-formyl-naphthyridyl-ureas derivatives as potential selective FGFR4 inhibitors: Design, synthesis, and biological activity studies. Bioorg Med Chem. 2019;: pubmed publisher
    ..When tested in mice, the representative compound 6f was found to have good pharmacokinetic parameters, low toxicity, and better tumor inhibiting activity in vivo. ..
  4. Hua S, Chen F, Wang X, Wang Y, Gou S. Pt(IV) hybrids containing a TDO inhibitor serve as potential anticancer immunomodulators. J Inorg Biochem. 2019;195:130-140 pubmed publisher
    ..Furthermore, complex 3 was effective to enhance T-cell immune responses by inhibiting the TDO enzyme expression to block the kynurenine production and inactivating the downstream of aryl hydrocarbon receptor (AHR). ..
  5. Chen H, Chen F, Pei S, Gou S. Pomalidomide hybrids act as proteolysis targeting chimeras: Synthesis, anticancer activity and B-Raf degradation. Bioorg Chem. 2019;87:191-199 pubmed publisher
    ..The anticancer mechanism of compound 2 is quite different from its mother compound and cancer cells seem to be more sensitive to the degrader, hinting that degradation of B-Raf by PROTAC is a potential way for cancer treatment. ..
  6. Hua S, Chen F, Xu G, Gou S. Multifunctional platinum(IV) complexes as immunostimulatory agents to promote cancer immunochemotherapy by inhibiting tryptophan-2,3-dioxygenase. Eur J Med Chem. 2019;169:29-41 pubmed publisher
    ..This immunochemotherapeutic strategy can be promisingly applied to treat with TDO-overexpressed cancers. ..
  7. Chen H, Wang X, Gou S. A cisplatin-based platinum(IV) prodrug containing a glutathione s-transferase inhibitor to reverse cisplatin-resistance in non-small cell lung cancer. J Inorg Biochem. 2019;193:133-142 pubmed publisher
    ..In vivo tests on A549 xenograft tumor mice model showed that complex 1 presented higher tumor inhibiting rate and lower toxicity than cisplatin as well. In all, the Pt(IV) prodrug has potential to be developed as an anticancer agent. ..
  8. Yang C, Wang L, Sun X, Tang M, Quan H, Zhang L, et al. SHR-A1403, a novel c-Met antibody-drug conjugate, exerts encouraging anti-tumor activity in c-Met-overexpressing models. Acta Pharmacol Sin. 2019;: pubmed publisher
    ..These data provide references for SHR-A1403 as a potential therapy for the treatment of cancers with c-Met overexpression. ..
  9. Chen H, Chen F, Liu N, Wang X, Gou S. Chemically induced degradation of CK2 by proteolysis targeting chimeras based on a ubiquitin-proteasome pathway. Bioorg Chem. 2018;81:536-544 pubmed publisher

More Information


  1. Zhang H, Gou S, Zhao J, Chen F, Xu G, Liu X. Cytotoxicity profile of novel sterically hindered platinum(II) complexes with (1R,2R)-N(1),N(2)-dibutyl-1,2-diaminocyclohexane. Eur J Med Chem. 2015;96:187-95 pubmed publisher
    ..Western blot analysis showed it had a similar apoptotic mechanism to cisplatin which could induce apoptosis via a mitochondrial-dependent pathway. ..
  2. request reprint
    Xu G, Lu H, Zhitao J, Zhang S, Gou S. Design, Synthesis and Biological Evaluation of Palladium (II) Complexes with 1-(substituted benzyl) azetidine-3,3-dicarboxylates as Leaving Group. Med Chem. 2015;11:701-7 pubmed
    ..The interaction between complex 12 and pET22b plasmid DNA was investigated by agarose gel electrophoresis, and the result of the study showed that complex 12 had no obvious interaction with the plasmid DNA. ..
  3. Hua W, Zhao J, Hu W, Gou S. Combination of 7-hydroxycoumarin in a platinum(IV) complex derived from cisplatin enhanced cytotoxicity with multiple mechanisms of action. J Inorg Biochem. 2018;186:17-23 pubmed publisher
    ..In vivo tests showed that Cou-platin, at equimolar dose to cisplatin, could inhibit tumor growth in nude mouse HCT116 tumor xenograft models almost as cisplatin and oxaliplatin, but with less toxicity. ..
  4. Li L, Huang X, Huang R, Gou S, Wang Z, Wang H. Pt(IV) prodrugs containing microtubule inhibitors displayed potent antitumor activity and ability to overcome cisplatin resistance. Eur J Med Chem. 2018;156:666-679 pubmed publisher
    ..Moreover, complex 19 significantly induced cell apoptosis and decreased MMP. Importantly, complex 19 significantly inhibited tumor growth in SK-OV-3 xenograft model in vivo without apparent toxicity. ..
  5. Lyu A, Fang L, Gou S. Design and synthesis of Lapatinib derivatives containing a branched side chain as HER1/HER2 targeting antitumor drug candidates. Eur J Med Chem. 2014;87:631-42 pubmed publisher
    ..Moreover, the pharmacokinetic investigation on 2i also indicated it had a good performance on both absorption and elimination profiles. ..
  6. Xu G, Zhao J, Gou S, Pang J. Antitumor platinum(II) complexes of N-cyclobutyl-1R,2R-diaminocyclohexane with dicarboxylates as leaving groups. Bioorg Med Chem Lett. 2015;25:221-4 pubmed publisher
    ..1μM). The DNA binding behavior of both complexes 3 and 4, studied by agarose gel electrophoresis, revealed that they bound to DNA in almost the same way as cisplatin. ..
  7. Huang X, Huang R, Wang Z, Li L, Gou S, Liao Z, et al. Pt(IV) complexes conjugating with chalcone analogue as inhibitors of microtubule polymerization exhibited selective inhibition in human cancer cells. Eur J Med Chem. 2018;146:435-450 pubmed publisher
    ..Molecular mechanism studies suggested that 14 and 17 induced production of reactive oxygen species (ROS), cell cycle arrest at the G2/M phase, and mitochondria-mediated apoptosis by regulating the expression of Bcl-2 family members. ..
  8. Huang X, Huang R, Liao Z, Pan Y, Gou S, Wang H. Synthesis and pharmacological evaluation of dehydroabietic acid thiourea derivatives containing bisphosphonate moiety as an inducer of apoptosis. Eur J Med Chem. 2016;108:381-391 pubmed publisher
    ..Furthermore, molecular docking studies showed that 6e could bind to the ATP pocket sites. ..
  9. Wang Z, Wu M, Gou S. Toward a better understanding of the oxaliplatin mode of action upon the steric hindrance of 1,2-diaminocyclohexane and its analogue. J Inorg Biochem. 2016;157:1-7 pubmed publisher
    ..2.2]octane-7,8-diamine possessing dicyclic steric hindrance, was also studied in the same way to explore its mode of action with DNA. ..
  10. Huang X, Hua S, Huang R, Liu Z, Gou S, Wang Z, et al. Dual-targeting antitumor hybrids derived from Pt(IV) species and millepachine analogues. Eur J Med Chem. 2018;148:1-25 pubmed publisher
    ..Our research provided an efficient strategy for multi-targeting antitumor drug development. ..
  11. Chen F, Jin X, Zhao J, Gou S. DN604: A platinum(II) drug candidate with classic SAR can induce apoptosis via suppressing CK2-mediated p-cdc25C subcellular localization in cancer cells. Exp Cell Res. 2018;364:68-83 pubmed publisher
  12. Hu W, Zhao J, Hua W, Gou S. A study on platinum(iv) species containing an estrogen receptor modulator to reverse tamoxifen resistance of breast cancer. Metallomics. 2018;10:346-359 pubmed publisher
  13. Chen H, Chen F, Hu W, Gou S. Effective platinum(IV) prodrugs conjugated with lonidamine as a functional group working on the mitochondria. J Inorg Biochem. 2018;180:119-128 pubmed publisher
    ..All the results provid evidence to support the design strategy of conjugating platinum complexes with its potentiator to improve their anticancer effect. ..
  14. Zhou Z, Chen F, Xu G, Gou S. Study on the cytotoxic activity of platinum(II) complexes of (1R,2R)-N(1)-cyclopentyl-1,2-cyclohexanediamine with substituted malonate derivatives. Bioorg Med Chem Lett. 2016;26:322-327 pubmed publisher
    ..Mechanism studies of cell proliferation inhibition and cellular uptake indicated that complex 2 entered HepG2 cell more efficiently than cisplatin, exhibited massive G2 accumulation and then induced apoptosis. ..
  15. Fang L, Chen M, Liu Z, Fang X, Gou S, Chen L. Ferulic acid-carbazole hybrid compounds: Combination of cholinesterase inhibition, antioxidant and neuroprotection as multifunctional anti-Alzheimer agents. Bioorg Med Chem. 2016;24:886-93 pubmed publisher
  16. Yu H, Gou S, Wang Z, Chen F, Fang L. Toward overcoming cisplatin resistance via sterically hindered platinum(II) complexes. Eur J Med Chem. 2016;114:141-52 pubmed publisher
    ..The steric hindrance resulting from a pending 2-fluorobenzyl moiety of the ligand might be the key factor for its ability to overcome cisplatin resistant cancer cells. ..
  17. Huang X, Huang R, Li L, Gou S, Wang H. Synthesis and biological evaluation of novel chalcone derivatives as a new class of microtubule destabilizing agents. Eur J Med Chem. 2017;132:11-25 pubmed publisher
    ..The results of tubulin polymerization assay displayed that 12k could inhibit tubulin polymerization in vitro. Furthermore, molecular docking study indicated that 12k can be binding to the colchicine site of tubulin. ..
  18. Zhao J, Fang L, Zhang X, Liang Y, Gou S. Synthesis and biological evaluation of new [1,2,4]triazolo[4,3-a]pyridine derivatives as potential c-Met inhibitors. Bioorg Med Chem. 2016;24:3483-93 pubmed publisher
  19. Xu Z, Hu W, Wang Z, Gou S. Platinum(IV) prodrugs multiply targeting genomic DNA, histone deacetylases and PARP-1. Eur J Med Chem. 2017;141:211-220 pubmed publisher
    ..Besides, HDACs inhibition activity and PARP-1 enzyme inhibition of SAA1 were also studied...
  20. Qin X, Fang L, Chen F, Gou S. Conjugation of platinum(IV) complexes with chlorambucil to overcome cisplatin resistance via a "joint action" mode toward DNA. Eur J Med Chem. 2017;137:167-175 pubmed publisher
    ..These results show that the "joint action" on DNA is an effective strategy to overcome cisplatin resistance. ..
  21. Zhao J, Wang D, Xu G, Gou S. Improve the anticancer potency of the platinum(II) complexes through functionalized leaving group. J Inorg Biochem. 2017;175:20-28 pubmed publisher
    ..Overall, the introduction of two methoxy groups to the skeleton of 1,1-cyclobutanedicarboxylate can not only change the kinetic reactivity of the resulting platinum(II) complexes, but also enhance their anticancer efficacy. ..
  22. Qin X, Xu G, Chen F, Fang L, Gou S. Novel platinum(IV) complexes conjugated with a wogonin derivative as multi-targeted anticancer agents. Bioorg Med Chem. 2017;25:2507-2517 pubmed publisher
    ..Overall, the research demonstrates that the "integrative" prodrug can be an effective strategy to promote the anticancer potency of Pt-based drugs for cancer treatment. ..
  23. Hu W, Fang L, Hua W, Gou S. Biotin-Pt (IV)-indomethacin hybrid: A targeting anticancer prodrug providing enhanced cancer cellular uptake and reversing cisplatin resistance. J Inorg Biochem. 2017;175:47-57 pubmed publisher
    ..hy926 cells. In all, this study offers a new strategy to enhance sensitivity and reduce toxicity of cisplatin. ..
  24. Huang X, Huang R, Gou S, Wang Z, Liao Z, Wang H. Platinum(IV) complexes conjugated with phenstatin analogue as inhibitors of microtubule polymerization and reverser of multidrug resistance. Bioorg Med Chem. 2017;25:4686-4700 pubmed publisher
    ..Moreover, complex 10 effectively inhibited the tumor growth in the NCI-H460 xenograft model. ..
  25. Chen F, Xu G, Qin X, Jin X, Gou S. Hybrid of DNA-targeting Chlorambucil with Pt(IV) Species to Reverse Drug Resistance. J Pharmacol Exp Ther. 2017;363:221-239 pubmed publisher
    ..Overall, compound 5 is a promising drug candidate, which could promote the anticancer activity and reverse drug resistance by attenuating CK2-induced MRN-dependent DSB repair. ..
  26. Zhao J, Hua W, Xu G, Gou S. Biotinylated platinum(IV) complexes designed to target cancer cells. J Inorg Biochem. 2017;176:175-180 pubmed publisher
    ..Further mechanistic studies on complex 1 indicated that it activated the expression of Bax, and induced cytochrome c release from the mitochondria, and finally activated caspase-3. ..
  27. Chen F, Huang X, Wu M, Gou S, Hu W. A CK2-targeted Pt(IV) prodrug to disrupt DNA damage response. Cancer Lett. 2017;385:168-178 pubmed publisher
    ..Further in vivo tests exhibited that Cx-platin displayed high tumor inhibition rates, increased weight gain, and hardly toxicity effects in contrast to cisplatin. ..
  28. Fang L, Feng M, Chen F, Liu X, Shen H, Zhao J, et al. Oleanolic acid-NO donor-platinum(II) trihybrid molecules: Targeting cytotoxicity on hepatoma cells with combined action mode and good safety. Bioorg Med Chem. 2016;24:4611-4619 pubmed publisher
    ..The flow cytometry studies found that 1c caused tumor apoptosis and blocked cell-cycle progression in the G2 phase. ..
  29. Chen F, Qin X, Xu G, Gou S, Jin X. Reversal of cisplatin resistance in human gastric cancer cells by a wogonin-conjugated Pt(IV) prodrug via attenuating Casein Kinase 2-mediated Nuclear Factor-?B pathways. Biochem Pharmacol. 2017;135:50-68 pubmed publisher