Affiliation: Southeast University
- 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. ..
- 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. ..
- 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. ..
- 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. ..
- 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. ..
- 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..1Î¼M). 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. ..
- 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. ..
- 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. ..
- 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. ..
- 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. ..
- 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. ..
- 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. ..
- 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. ..
- 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. ..
- 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...
- 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. ..
- 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. ..
- 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. ..
- 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. ..
- 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. ..
- 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. ..
- 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. ..
- 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. ..
- 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. ..