Synthesis and crystal structure of chalcones as well as on cytotoxicity and antibacterial properties

被引：29
作者：
Wu, Jianzhang [1 ,2 ]
Wang, Cong [1 ,3 ]
Cai, Yuepiao [1 ]
Peng, Jing [1 ]
Liang, Donglou [1 ]
Zhao, Yunjie [1 ]
Yang, Shulin [2 ]
Li, Xiaokun [1 ,2 ]
Wu, Xiaoping [1 ,3 ]
Liang, Guang [1 ,2 ]
机构：
[1] Wenzhou Med Coll, Sch Pharm, Bioorgan & Med Chem Res Ctr, Wenzhou 325035, Zhejiang, Peoples R China
[2] Nanjing Univ Sci & Technol, Inst Biotechnol, Nanjing 210094, Jiangsu, Peoples R China
[3] Jinan Univ, Inst Tissue Transplantat & Immunol, Guangzhou 510632, Guangdong, Peoples R China
来源：
MEDICINAL CHEMISTRY RESEARCH | 2012年 / 21卷 / 04期
关键词：
Chalcones; Synthesis; Cytotoxicity; Antibacterial activity; Crystal structure; IN-VITRO; DERIVATIVES; MACROPHAGES; INDUCTION; ANALOGS; DESIGN; AGENTS;
D O I：
10.1007/s00044-011-9549-9
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A series of chalcones derivatives were synthesized and evaluated for cytotoxic and antibacterial activities in vitro. These modifications changed their bioactivity profile and indicated a combination of SAR analysis toward the substituents in rings A and B of chalcones. Compounds 2, 6-8, 14-17, and 32 exhibited good cytotoxic properties against two human cancer cell lines HT29 and SGC7901. Compounds 16 and 17 showed high antibacterial activity toward 14 clinically isolated multidrug-resistant strains. Subsequently, the structure of bi-bioactive compound 16 was determined using single-crystal X-ray diffraction. This study presents a few novel leading compounds for the development of potential antitumor and antibacterial agents.
引用
收藏
页码：444 / 452
页数：9
相关论文
共 50 条
  • [21] Synthesis and Evaluation of Antibacterial Properties of Chalcones Derived from Thiophene-2-Carbaldehyde
    Shetty, Chaithra R.
    Dikshith, L.
    Dsouza, Fathima Sible
    Shahana, Fathimath
    Nooha, Fatima
    JOURNAL OF PHARMACEUTICAL RESEARCH INTERNATIONAL, 2021, 33 (55A) : 72 - 79
  • [22] Synthesis and pharmacological properties of coumarin-chalcones
    Bensalah, Donia
    Amri, Nasser
    Mukhrish, Yousef E.
    Koko, Waleed S.
    Hamdi, Naceur
    METHODSX, 2023, 11
  • [23] Heteroaryl Chalcones: Design, Synthesis, X-ray Crystal Structures and Biological Evaluation
    Kumar, C. S. Chidan
    Loh, Wan-Sin
    Ooi, Chin Wei
    Quah, Ching Kheng
    Fun, Hoong-Kun
    MOLECULES, 2013, 18 (10) : 12707 - 12724
  • [24] Efficient Synthesis, Crystal Structure and Antibacterial Activity of Two Novel 1,3-Oxazin Derivatives
    Yu Yun
    He Jia-Xin
    Hu Hui-Ling
    Lin Zhi-Lan
    Gao Yuan
    CHINESE JOURNAL OF STRUCTURAL CHEMISTRY, 2014, 33 (03) : 441 - 447
  • [25] Synthesis, crystal structure and antibacterial studies of 2,4,6-trimetoxybenzaldehyde based dihydropyrimidine derivatives
    Huseynzada, A. E.
    Jelsch, C.
    Akhundzada, H. N.
    Soudani, S.
    Ben Nasr, C.
    Doria, F.
    Hasanova, U. A.
    Freccero, M.
    Gakhramanova, Z.
    Ganbarov, K.
    Najafov, B.
    JOURNAL OF MOLECULAR STRUCTURE, 2021, 1241
  • [26] Synthesis, Characterization and Antibacterial Activities of New Fluorinated Chalcones
    Kayode L. Amole
    Isaac A. Bello
    Adebayo O. Oyewale
    Chemistry Africa, 2019, 2 : 47 - 55
  • [27] Synthesis, crystal structure, and antibacterial activity of tricyclohexyltin salicylates
    Zhang, Shuai
    Wang, Wenqiang
    Liu, Qingtao
    Zheng, Xiaofeng
    Tian, Laijin
    MAIN GROUP METAL CHEMISTRY, 2016, 39 (3-4) : 87 - 92
  • [28] Tin(IV) Complexes with Salen Type Schiff Base: Synthesis, Spectroscopic Characterization, Crystal Structure, Antibacterial Screening and Cytotoxicity
    Ali, S.
    Ara, T.
    Danish, M.
    Shujah, S.
    Slawin, A. M. Z.
    RUSSIAN JOURNAL OF COORDINATION CHEMISTRY, 2019, 45 (12) : 889 - 898
  • [29] Tin(IV) Complexes with Salen Type Schiff base: Synthesis, Spectroscopic Characterization, Crystal Structure, Antibacterial Screening and Cytotoxicity
    S. Ali
    T. Ara
    M. Danish
    S. Shujah
    A. M. Z. Slawin
    Russian Journal of Coordination Chemistry, 2019, 45 : 889 - 898
  • [30] Synthesis, Characterization and Antibacterial Activities of New Fluorinated Chalcones
    Amole, Kayode L.
    Bello, Isaac A.
    Oyewale, Adebayo O.
    CHEMISTRY AFRICA-A JOURNAL OF THE TUNISIAN CHEMICAL SOCIETY, 2019, 2 (01): : 47 - 55
12345