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Chinese Journal of Chemistry 2022年第12期40卷 1447-1456页

作者： Jianlin Lv Yajun Xu Yue Huang Haiyang Yu Zhaohui Tang Key Laboratory of Polymer Ecomaterials Changchun Institute of Applied ChemistryChinese Academy of SciencesChangchunJilin 130022China School of Applied Chemistry and Engineering University of Science and Technology of ChinaHefeiAnhui 230026China Jilin Biomedical Polymers Engineering Laboratory 5625 Renmin StreetChangchunJilin 130022China

This work was supported by the National Natural Science Foundation of China(Nos.52025035,52103195).The comprehensive graphic content and graphic abstract were created with *** by coauthors.

关键词： Vascular disrupting agents antitumor agents Self-assembly Cancer Nanoparticles

Cation-anionicpalladium Complexes—New Types of antitumor, Immune Response-modulating and Radioprotective agents

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贵金属 2012年第A1期33卷 240-242页

作者： EFIMENKO I.A. SHISHILOV O.N. IVANOVA N.A. EROFEEVA O.S. N.S. Kurnakov Institute of General and Inorganic Chemistry of RAS MoscowRussia

Here we report results of our investigations of new class of bioactive palladium compounds (AH n ) m [PdCl 4 ], which were discovered as a result of systematic study of correlations between composition, structure and bioactivity of different types of platinum metals coordination compounds. For the first time we demonstrated in vivoa possibility of development of palladium compounds, which exceed cisplatin in antitumor activity and do not show immunosuppressive effects, and palladium compounds with immunostimulating and radioprotective activities. Combinations of cytostatic agents or radiation with palladium complexes lead to significant synergism of their activities and high therapeutic efficiency exceeded an efficiency of their separated use.

关键词： palladium chlorides heterocyclic amines antitumor agents immune response-modulating agents radioprotective agents

Photothermally Enhanced Dual Enzyme-mimic Activity of Gold-Palladium Hybrid Nanozyme for Cancer Therapy

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Chinese Journal of Chemistry 2023年第23期41卷 3189-3196页

作者： Yan Kang Chao Li Huali Shi Amin Zhang Chusen Huang Chaohui Zhou Nengqin Jia The Education Ministry Key Lab of Resource Chemistry Joint International Research Laboratory of Resource ChemistryShanghai Key Laboratory of Rare Earth Functional MaterialsCollege of Chemistry and Materials ScienceShanghai Normal University100 Guilin RDShanghai200234 China Institute of Nano Biomedicine and Engineering Shanghai Engineering Research Center for Intelligent Diagnosis and Treatment InstrumentDepartment of Instrument Science and EngineeringSchool of Electronic Information and Electrical EngineeringShanghai Jiao Tong University800 Dongchuan RDShanghai200240 China

Based on characteristics of the tumor microenvironment(TME),including acidity,hypoxia,inflammation and hydrogen peroxide overload,combined with emerging nanotechnologies,designing nanoplatforms with TME specificity/responsiveness for tumor treatment is a promising nanotherapeutic *** this work,a multifunctional gold-palladium bimetallic cascade nanozyme was constructed for effective photothermal-enhanced cascade catalyzed synergistic therapy of *** dumbbell-like Au-Pd bimetallic nanomaterial(Au NRs-Pd@HA)was obtained by reducing palladium on gold nanorods with ascorbic acid(AA)and further modified with hyaluronic acid(HA).The introduction of HA brings biocompatibility and targeting *** zebrafish embryos model showed that Au NRs-Pd@HA had good biocompatibility and low *** NRs-Pd@HA can induce catalytic conversion of glucose to generate H_(2)O_(2) efficiently,and subsequently undergo cascade reaction to produce abundant·OH radicals,exhibiting peroxidase-like(POD-like)and glucose oxidase-like(GOD-like)*** generated·OH was a key factor for tumor ***,Au NRs-Pd@HA exhibits good photothermal performance under 808 nm irradiation,in favor of photothermal therapy(PTT).Especially,the POD-like and GOD-like activities were significantly enhanced due to the photothermal *** synergistic PTT and photothermal-enhanced nanozymes with cascade catalytic effect enabled efficient and safe cancer therapy.

关键词： Nanozymes catalyzed therapy Photothermal therapy Cascade catalytic Good biocompatibility Cancer antitumor agents Catalytic therapy

Lithocarpins E-G, Potent Anti-Tumor Tenellone-Macrolides from the Deep-Sea Fungus Phomopsis lithocarpus FS508

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Chinese Journal of Chemistry 2021年第5期39卷 1104-1112页

作者： Jianlin Xu Yuchan Chen Zhaoming Liu Saini Li Yong Wang Yuhong Ren Hongxin Liu Weimin Zhang State Key Laboratory of Applied Microbiology Southern China Guangdong Provincial Key Laboratory of Microbiol Culture Collection and ApplicationGuangdong Open Laboratory of Applied MicrobiologyGuangdong Institute of MicrobiologyGuangdong Academy of SciencesGuangzhouGuangdong 510070China State Key Laboratory of Bioreactor Engineering East China University of Science and TechnologyShanghai 200237China Key Laboratory of Synthetic Biology CAS Center for Excellence in Molecular Plant SciencesInstitute of Plant Physiology and EcologyChinese Academy of SciencesShanghai 200032China

Lithocarpins E-G,featuring a rare naturally-occurring highly oxygenated tenellone-macrolide skeleton,were isolated from the culture extract of a marine-derived fungus Phomopsis lithocarpus *** structures were fully elucidated by NMR and MS spectroscopic analyses and electronic circular dichroism *** 1-3 were evaluated for their in vitro cytotoxicities against HepG2,MCF-7,SF-268,as well as A549 cell lines,among which,compound 1 exhibited inhibitory activity against HepG2 cells with an IC_(50) value of 6.3 μmol/*** further mechanistic investigation demonstrated that lithocarpin E could cause the apoptosis of HepG2 cells through activation of p-ERK,Bax,and caspase-3 gene expressions.

关键词： Phomopsis lithocarpus FS508 Polyketides Structure elucidation antitumor agents Apoptosis

Design, Synthesis and Preliminary Biological Evaluation of Purine-2,6-diamine Derivatives as Cyclin-dependent Kinase （CDK） Inhibitors

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Chinese Journal of Chemistry 2013年第9期31卷 1181-1191页

作者： Junhua Wang Quande Wang Liangren Zhang Hao Fang Department of Medicinal Chemistry School of Pharmaceutical Sciences Shandong University Jinan Shandong 250012 China State Key Laboratory of Natural and Biomimetic Drugs School of Pharmaceutical Sciences Peking University Beijing 100191 China

Novel purine-2,6-diamine derivatives were designed and synthesized as cyclin-dependent kinase （CDK） inhibi- tors. According to the preliminary biological evaluation, most of the compounds show good inhibitory activities in CDK1 enzyme assay and potent antiproliferative activities in some tumor cell lines. Especially, compound lla （IC50=0.35 μmol/L for CDK1/cyclin B and IC50： effect compared with Roscovitine （IC50= 2.54 CDK2/cyclin A）. 0.023 μmol/L for CDK2/cyclin A） possessed better inhibitory μmol/L for CDK1/cyclin B and IC50=0.092 μ mol/L for

关键词： purine derivatives CDK inhibitors antitumor agents regulation of cell cycle

Total Synthesis and Stereochemical Assignment of Talaroconvolutin A and Talarofuranone: Gram-scale Synthesis of Ferroptosis Inducer Talaroconvolutin A

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Chinese Journal of Chemistry 2024年第13期42卷 1509-1514页

作者： Ming Yao Wei Yang Jing Li Chengyun Huang Jin Fang Sulu Qin Shuzhi Liu Xiaolong Yang School of Pharmaceutical Sciences South-Central Minzu UniversityWuhanHubei 430074China

The first total synthesis of talaroconvolutin A(1.1 g obtained)and talarofuranone has been achieved using accessible materials(12 steps,7.5%and 8.2%yields,respectively).Convergent routes involved intramolecular Diels-Alder reactions in two approaches for creating the decalin ***,an unprecedented DMP-mediated domino reaction resulted in the deoxy-tetramic acid *** syntheses not only establish the absolute configuration of talaroconvolutin A but also enable further collaborative studies of this typeofferroptosisinducers.

关键词： Natural products Aldehydes Total synthesis Domino reactions Biological activity antitumor agents Ferroptosis Diels-Alder reaction Talaroconvolutin A

Preparation of Platinum(II) Complexes with 1-β-D-Ribofuranosyl-1,2,4-triazole-3-carboxamide and its Deoxy-analogue

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Chinese Chemical Letters 2001年第6期12卷 559-562页

作者： Wen PEI Kobe JOZE College of Chemical Engineering Zhejiang University of TechnologyHangzhou 310014 National Institute of Chemistry Hajdrihova 19SI-1115 LjubljanaSlovenia

The platinum (II) complexes of the [Pt (N4,N7-Ribavirin) (DMSO) Cl], [Pt (N4,N7-De-oxyribavirin) (DMSO) Cl] were obtained by the reactions of cis-[Pt (DMSO)2 Cl2] and K[Pt (DMSO) Cl3] with 1-??-D-ribofuranosyl-1,2,4-triazole-3-carboxamide (Ribavirin) and its deoxy-analogue (deoxyribavirin). The preparation of 1-(2'-deoxy-?-D-ribofuranosyl) -1,2,4-triazole-3-carboxamide was also performed through a four-step procedure, protection of 3', 5'-dihydroxyl group of Ribavirin with 1,3-dichloro-1,1,3,3-tetraisopropyldisiloxane (TPDS-Cl), phenoxythio-carbonylation of the 2'-hydroxyl group of 3', 5'-O-TPDS-Ribavirin with phenoxythiocarbonyl-chloride (PTC-Cl), reduction of 2′-O-phenoxythiocarbonyl ester of 3', 5'-O-TPDS-Ribavirin with tri-n-butyltin hydride and AIBN, deprotection of 3', 5'-O-TPDS-Ribavirin with tetrabutylammon-ium fluoride in THF.

关键词： Platinum(II) complexes ribavirin and deoxyribavirin nucleobase platination complexation reaction antitumor agents

In silico design of anti-tumor mini-protein targeting MDM2

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Chinese Chemical Letters 2023年第5期34卷 256-258页

作者： Jinghui Zhang Huixin Xu Baishi Wang Xuekai Zhang Lei Fu Yannan Li Guanzhao Wu Zitong Zhao Lu Liu Ting Yang Zheyu Zhang Jinbo Yang Tao Jiang Peiju Qiu Rilei Yu Key Laboratory of Marine Drugs Chinese Ministry of EducationSchool of Medicine and PharmacyOcean University of ChinaQingdao 266003China Laboratory for Marine Drugs and Bioproducts of Qingdao National Laboratory for Marine Science and Technology Qingdao 266237China Innovation Center for Marine Drug Screening&Evaluation Pilot National Laboratory for Marine Science and Technology(Qingdao) Qingdao 266003China Department of Biological Engineering College of Chemical and Biological EngineeringShandong University of Science and TechnologyQingdao 266590China

We designed a disulfide-crosslinked mini-protein with a two-helical topology consisting of L-and Damino acids,which was exceptionally stable in ***,we further used it as a scaffold to design mini-proteins targeting p53 positive tumor *** on bifunctional grafting,key residues from the transactivation domain of p53 and a designed unnatural amino acid were grafted into the helix constituted by L-amino acids to confer the mini-protein with MDM2 inhibitory ***,ten Arg residues were introduced to improve its membrane penetrating *** the mini-proteins,UPROL-10e showed nano-molar binding affinity on MDM2 and cellular toxicity on p53 expressing HCT116cells.

关键词： Protein design antitumor agents In silico design Constrained peptide Epitope grafting

Precise Control of Self-assembly in vivo Based on Polymer-Peptide Conjugates

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Chinese Journal of Chemistry 2022年第23期40卷 2815-2824页

作者： Yin-Sheng Xu Hao Wang Zeng-Ying Qiao CAS Key Laboratory for Biomedical Effects of Nanomaterials and Nanosafety CAS Center for Excellence in NanoscienceNational Center for Nanoscience and Technology(NCNST)Center of Materials Science and Optoelectronics EngineeringUniversity of Chinese Academy of SciencesBeijing 100190China

The self-assembled nanomaterials based on peptides,which have not only good biocompatibility and low toxicity but also high stability and performance,are increasingly becoming an important way for cancer *** this review,we highlight the progress of in vivo self-assembled polymer-peptide conjugates(PPCs)and their application,showing the recent advances in the development of“in vivo self-assembly”strategy for cancer *** the diverse microenvironments of tumor cells,different responsive assembly strategies(enzyme,pH,redox,temperature,etc.)have been developed to precisely control the assembly at different biological levels,realizing enhanced drug delivery and improved anticancer efficacy.

关键词： Polymer-peptide conjugates Drug design In vivo self-assembly Drug delivery antitumor agents

Yeast-Controlled Double-Shelled CacO_(3)/CaF_(2)Hollow Nanospheres with Hierarchically Porous for Sustained pH-Sensitive Drug Release

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Chinese Journal of Chemistry 2024年第15期42卷 1713-1720页

作者： Xinhe Liu Yi Chang Guanglei Ma Tingting Liu Penghui Song Heng Yu Xueqing Ren Yuming Guo Xiaoming Ma School of Chemistry and Chemical Engineering Henan Normal UniversityXinxiangHenan 453007China Collaborative Innovation Center of Henan Province for Green Manufacturing of Fine Chemicals Key Laboratory of Green Chemical Media and ReactionsMinistryof EducationHenan Normal UniversityXinxiangHenan 453007China

Hierarchically porous materials(HP materials)are believed one of the most hopeful matrix materials because of their distinctive multimodal pore structures and tremendous application potentials in the field of ***,green and facile synthesis of hierarchically porous nanomaterials with beneficial water dispersibility and biocompatibility is still a great ***,a novel biomimetic strategy is proposed to prepare the cell-tailored double-shelled HPCaCO_(3)/CaF_(2) hollow nanospheres under the mediation of yeast *** biomolecules derived from the secretion of yeast cells are used as conditioning and stabilizing agents to control the biosynthesis of the HPCaCO_(3)/CaF_(2) materials,which exhibit excellent water dispersibility and favorable *** double-shelled CaCO_(3)/CaF_(2) nanospheres hold hierarchically porous structure and have abundant pore channel and large specific surface area,showing high drug-loading and a prolonged drug sustainable release profile by the pore-by-pore diffusion pattern of the hierarchical ***,the HPCaCO_(3) with pH-sensitivity could controllably release drug doxorubicin hydrochloride(DOX)at the acidic tumor *** in vitro and in vivo results demonstrate that HPCaCO_(3)/CaF_(2) has the sustainable pH-sensitive drug release property,showing an enhanced therapeutic ***,this study provides a biomimetic strategy to synthesize the hierarchically porous double-shelled hollow nanomaterials for applying in sustainable drug delivery system.

关键词： Biomimetic synthesis Hierarchically porous Sustained pH-sensitive drug release antitumor agents Drug delivery Calcium Cancer therapy/Hollow structures