Novel 3-(1-acetyl-5-(substituted-phenyl)-4,5-dihydro-1H-pyrazol-3-yl)-7-fluoro-2H-chromen-2-one Derivatives: Synthesis and Anticancer Activity

被引：17
|
作者：
Cai, Zheng-Yu [1 ]
Yang, Yang [1 ]
Liu, Xin-Hua [1 ]
Qi, Xing-Bao [2 ]
机构：
[1] Anhui Univ Technol, Sch Chem & Chem Engn, Maanshan 243002, Peoples R China
[2] China Pharmaceut Univ, Sch Pharm, Nanjing 210009, Peoples R China
来源：
LETTERS IN DRUG DESIGN & DISCOVERY | 2010年 / 7卷 / 09期
基金：
中国国家自然科学基金;
关键词：
Coumarin; Dihydropyrazole; Molecular Docking; Antitumor Agent; ANTIBACTERIAL ACTIVITY;
D O I：
10.2174/157018010792929540
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A series of novel coumarin derivatives containing 4,5-dihydropyrazole moiety as potential telomerase inhibitors were synthesized. The bioassay tests showed that compound 3b exhibited potentially high activity against human gastric cancer cell SGC-7901 with IC50 value was 2.98 +/- 0.16. Docking simulation was performed to position compound 3b into the telomerase (3DU6) active site to determine the probable binding model. The result shows that some coumarin containing 4,5-dihydropyrazole moiety can combine well with the telomerase active site and may have use as potential telomerase inhibitors.
引用
收藏
页码：640 / 643
页数：4
相关论文
共 50 条
  • [41] Synthesis and pharmacological activities of some novel 5-chloro-N-(4-(1,5-(disubstituted)-4,5-dihydro-1H-pyrazol-3-yl)phenyl)-2-methoxybenzamide derivatives
    Mohamed M. Abdulla
    Abd El-Galil E. Amr
    Mohamed A. Al-Omar
    Azza A. Hussain
    Ahmed F. A. Shalaby
    Medicinal Chemistry Research, 2014, 23 : 2113 - 2121
  • [42] Synthesis and pharmacological activities of some novel 5-chloro-N-(4-(1,5-(disubstituted)-4,5-dihydro-1H-pyrazol-3-yl)phenyl)-2-methoxybenzamide derivatives
    Abdulla, Mohamed M.
    Amr, Abd El-Galil E.
    Al-Omar, Mohamed A.
    Hussain, Azza A.
    Shalaby, Ahmed F. A.
    MEDICINAL CHEMISTRY RESEARCH, 2014, 23 (04) : 2113 - 2121
  • [43] Synthesis, Crystal Structure and Recognition Properties of 2-(5-(4-Chlorophenyl)-1-phenyl-4,5-dihydro-1H-pyrazol-3-yl)pyridine
    钟立群
    张姝姝
    陶清
    胡胜利
    Chinese Journal of Structural Chemistry, 2014, (05) : 779 - 784
  • [44] Synthesis, Crystal Structure and Recognition Properties of 2-(5-(4-Chlorophenyl)-1-phenyl-4,5-dihydro-1H-pyrazol-3-yl)pyridine
    钟立群
    张姝姝
    陶清
    胡胜利
    结构化学, 2014, 33 (05) : 779 - 784
  • [45] Synthesis, Crystal Structure and Recognition Properties of 2-(5-(4-Chlorophenyl)-1-phenyl-4,5-dihydro-1H-pyrazol-3-yl)pyridine
    Zhong Li-Qun
    Zhang Shu-Shu
    Tao Qing
    Hu Sheng-Li
    CHINESE JOURNAL OF STRUCTURAL CHEMISTRY, 2014, 33 (05) : 779 - 784
  • [46] Synthesis of novel 3-(4-acetyl-5H/methyl-5-substituted phenyl-4,5-dihydro-1,3,4-oxadiazol-2-yl)-2H-chromen-2-ones as potential anticonvulsant agents
    Bhat, Mashooq A.
    Siddiqui, Nadeem
    Khan, Suroor A.
    ACTA POLONIAE PHARMACEUTICA, 2008, 65 (02): : 235 - 239
  • [47] 6-Chloro-3-[5-(4-fluorophenyl)-1-phenyl-4,5-dihydro-1H-pyrazol-3-yl]-2-methyl-4-phenylquinoline
    Loh, Wan-Sin
    Fun, Hoong-Kun
    Sarveswari, S.
    Vijayakumar, V.
    Reddy, B. Palakshi
    ACTA CRYSTALLOGRAPHICA SECTION E-STRUCTURE REPORTS ONLINE, 2010, 66 : O304 - U1919
  • [48] Synthesis of 2-(3-methyl-5-oxo-4,5-dihydro-1H-pyrazol-1-yl) quinazolin-4(3H)-one derivatives
    Bireddy, Srinivasa Reddy
    Rafeeq, Mohammad
    Chittireddy, Venkata Ramana Reddy
    VIETNAM JOURNAL OF CHEMISTRY, 2021, 59 (01) : 73 - 78
  • [49] Synthesis and evaluation of in vitro antiviral activity of 2-[3-(substituted phenyl)-4,5-dihydro-1H-5-pyrazolyl]benzofuran-3-yl chloride derivatives
    Yar, A. Shahar
    Abdullah, M. Mustaqeem
    Husain, A.
    Bhakht, M. Afroz
    De Clercq, Erik
    JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, 2009, 24 (04) : 949 - 956
  • [50] Crystal structure of 2-(5-phenyl-1-(quinolin-2-yl)-4,5-dihydro-1H-pyrazol-3-yl)phenol, C24H19N3O
    Zeng, Dai
    Tan, Kai
    Fang, Ziyan
    Xing, Aiping
    ZEITSCHRIFT FUR KRISTALLOGRAPHIE-NEW CRYSTAL STRUCTURES, 2023, 238 (06): : 1153 - 1155
12345