Novel Bis-Artemisinin-Phloroglucinol hybrid molecules with dual anticancer and immunomodulatory Activities: Synthesis and evaluation

被引：1
|
作者：
Xu, Wei [1 ]
Zou, Xiaosu [2 ]
Zha, Yufeng [3 ]
Zhang, Jinghua [1 ]
Bian, Hongzhu [3 ]
Shen, Zhengwu [1 ,2 ]
机构：
[1] Shanghai Jiao Tong Univ, Sch Med, 280 South Chongqing Rd, Shanghai 200025, Peoples R China
[2] Shanghai Univ Tradit Chinese Med, Sch Pharm, 1200 Cai Lun Rd, Shanghai 201203, Peoples R China
[3] Yunnan Baiyao Grp Co Ltd, 3686 Yunnan Baiyao St, Kunming 650200, Peoples R China
来源：
BIOORGANIC CHEMISTRY | 2023年 / 139卷
基金：
中国国家自然科学基金;
关键词：
Artemisinin; Dimer; Anticancer; Immunosuppression; IMMUNOSUPPRESSIVE ACTIVITY; QINGHAOSU ARTEMISININ; ANTIVIRAL ACTIVITIES; IN-VITRO; ANTIMALARIAL; DERIVATIVES; CANCER; DIMERS; CYTOTOXICITY; MECHANISMS;
D O I：
10.1016/j.bioorg.2023.106705
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
Bis-(10-deoxydihydroartemisinin)-phloroglucinol (9), has been synthesized in a one-step reaction and has demonstrated strong inhibition to cancer cell proliferation and immunosuppressive activity. The structure modification of the compound reduced its cytotoxicity, and among the analogs, bis-(10-deoxydihydroartemisinin)-phloroglucinol phenyl decanoate (16) showed significant reduction of ear swelling in a mouse model for DNFB-induced delayed-type hypersensitivity without observable toxicity in a dose-dependent manner.
引用
收藏
页数：13
相关论文
共 50 条
  • [21] Synthesis and biological evaluation of novel bisphosphonates with dual activities on bone in vitro
    Xie, YL
    Ding, HS
    Qian, LH
    Yan, XM
    Yang, CH
    Xie, YY
    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2005, 15 (13) : 3267 - 3270
  • [22] Synthesis of novel bis-thiazoles, bis-thienopyridines, and bis-triazolothiadiazines linked to diphenyl ether core as novel hybrid molecules
    Elwahy, Ahmed H. M.
    Ginidi, Ahmed R. S.
    Shaaban, Mohamed R.
    Farag, Ahmed M.
    Salem, Mostafa E.
    SYNTHETIC COMMUNICATIONS, 2023, 53 (05) : 426 - 441
  • [23] Design, synthesis, and biological evaluation of novel artemisinin-based HDAC inhibitors with antitumor and antimalarial activities
    He, Jin
    He, Youyou
    Qian, Yunan
    Du, Shuaibo
    Sun, Ruikang
    Liu, Yujiao
    Yu, Jiping
    Ding, Yi
    Zhou, Siyuan
    Jiang, Lubin
    Wang, Shengzheng
    BIOORGANIC CHEMISTRY, 2025, 157
  • [24] Synthesis of Novel Lipophilic N-Substituted Norcantharimide Derivatives and Evaluation of Their Anticancer Activities
    Wu, Jin-Yi
    Kuo, Cheng-Deng
    Chu, Chien-Yu
    Chen, Min-Shin
    Lin, Jia-Hua
    Chen, Yu-Jen
    Liao, Hui-Fen
    MOLECULES, 2014, 19 (06) : 6911 - 6928
  • [25] Novel Hybrid Molecules of Quinazoline Chalcone Derivatives: Synthesis and Study of In Vitro Cytotoxic Activities
    Thiriveedhi, Arunkumar
    Nadh, Ratnakaram Venkata
    Srinivasu, Navuluri
    Kaushal, Kishore
    LETTERS IN DRUG DESIGN & DISCOVERY, 2018, 15 (07) : 757 - 765
  • [26] Novel Hybrid Molecules of Isoxazole Chalcone Derivatives: Synthesis and Study of In Vitro Cytotoxic Activities
    Thiriveedhi, Arunkumar
    Nadh, Ratnakaram Venkata
    Srinivasu, Navuluri
    Kaushal, Kishore
    LETTERS IN DRUG DESIGN & DISCOVERY, 2018, 15 (06) : 576 - 582
  • [27] Design, synthesis and anticancer evaluation of novel spirobenzo[h]chromene and spirochromane derivatives with dual EGFR and B-RAF inhibitory activities
    Abdelatef, Shaimaa A.
    El-Saadi, Mohammed T.
    Amin, Noha H.
    Abdelazeem, Ahmed H.
    Omar, Hany A.
    Abdellatif, Khaled R. A.
    EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2018, 150 : 567 - 578
  • [28] Synthesis of novel bis- and poly(hydrazinylthiazole) linked to benzofuran or benzothiazole as new hybrid molecules
    Salem, Mostafa E.
    Darweesh, Ahmed F.
    Shaaban, Mohamed R.
    Elwahy, Ahmed H. M.
    ARKIVOC, 2019, : 73 - 88
  • [29] Synthesis of novel scaffolds based on bis-thiazole or bis-triazolothiadiazine linked to quinoxaline as new hybrid molecules
    Salem, Mostafa E. E.
    Qenawy, Mohmmad S. S.
    Farag, Ahmed M. M.
    Elwahy, Ahmed H. M.
    SYNTHETIC COMMUNICATIONS, 2023, 53 (02) : 103 - 118
  • [30] Novel Hybrid Compounds Containing Benzofuroxan and Aminothiazole Scaffolds: Synthesis and Evaluation of Their Anticancer Activity
    Chugunova, Elena
    Micheletti, Gabriele
    Telese, Dario
    Boga, Carla
    Islamov, Daut
    Usachev, Konstantin
    Burilov, Alexander
    Tulesinova, Alena
    Voloshina, Alexandra
    Lyubina, Anna
    Amerhanova, Syumbelya
    Gerasimova, Tatiana
    Gilfanova, Aisylu
    Syakaev, Victor
    INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES, 2021, 22 (14)
12345