Synthesis of new pyrazole derivatives and their anticancer evaluation

被引：98
|
作者：
Nitulescu, George Mihai [1 ]
Draghici, Constantin [2 ]
Missir, Alexandru Vasile [1 ]
机构：
[1] Carol Davila Univ Med & Pharm, Fac Pharm, Dept Pharmaceut Chem, Bucharest 020956, Romania
[2] Romanian Acad Costin D Nenitescu, Organ Chem Ctr, Bucharest 060023, Romania
来源：
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2010年 / 45卷 / 11期
关键词：
1-Methyl-1H-pyrazole-4-carboxylic acid; Acyl thiourea; Thiazolylidenes; Anticancer activity; Pyrazole amines; NATIONAL-CANCER-INSTITUTE; TUMOR-CELL-LINES; ANTITUMOR AGENTS; CDK INHIBITORS; DRUG DISCOVERY; KINASE;
D O I：
10.1016/j.ejmech.2010.07.064
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A series of functionally substituted pyrazole compounds have been synthesized and evaluated in vitro for their antiproliferative effects on a panel of 60 cellular lines, according to the National Cancer Institute screening protocol. Three of the 12 tested compounds showed moderate antitumor activity, one of them being chosen for the 5-dose assay and presented logGl(50) values up to -5.75. (C) 2010 Elsevier Masson SAS. All rights reserved.
引用
收藏
页码：4914 / 4919
页数：6
相关论文
共 50 条
  • [1] Synthesis, structural characterization and anticancer evaluation of pyrazole derivatives
    El-Gaby, Mohamed S. A.
    Ghorab, Mustafa M.
    Ismail, Zainb H.
    Abdel-Gawad, Soad. M.
    Aly, Hala. M.
    MEDICINAL CHEMISTRY RESEARCH, 2018, 27 (01) : 72 - 79
  • [2] Synthesis and anticancer evaluation of novel isoxazole/pyrazole derivatives
    Sherifa M. Abu Bakr
    Somaia S. Abd El-Karim
    Medhat M. Said
    Mahmoud M. Youns
    Research on Chemical Intermediates, 2016, 42 : 1387 - 1399
  • [3] Synthesis, structural characterization and anticancer evaluation of pyrazole derivatives
    Mohamed S. A. El-Gaby
    Mustafa M. Ghorab
    Zainb H. Ismail
    Soad. M. Abdel-Gawad
    Hala. M. Aly
    Medicinal Chemistry Research, 2018, 27 : 72 - 79
  • [4] Synthesis and anticancer evaluation of novel isoxazole/pyrazole derivatives
    Abu Bakr, Sherifa M.
    Abd El-Karim, Somaia S.
    Said, Medhat M.
    Youns, Mahmoud M.
    RESEARCH ON CHEMICAL INTERMEDIATES, 2016, 42 (02) : 1387 - 1399
  • [5] Design, Synthesis, and Anticancer Evaluation of New Coumarin and Pyrazole Derivatives Bearing Benzenesulfonamide Moiety
    Elgogary, Sameh R.
    El-Telbani, Emad M.
    INDIAN JOURNAL OF HETEROCYCLIC CHEMISTRY, 2023, 33 (02) : 199 - 207
  • [6] Synthesis and biological evaluation of novel pyrazole derivatives with anticancer activity
    Balbi, Alessandro
    Anzaldi, Maria
    Maccio, Chiara
    Aiello, Cinzia
    Mazzei, Mauro
    Gangemi, Rosaria
    Castagnola, Patrizio
    Miele, Mariangela
    Rosano, Camillo
    Viale, Maurizio
    EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2011, 46 (11) : 5293 - 5309
  • [7] Synthesis, Anticancer Activity, and Computational Studies of New Pyrazole Derivatives
    Khairulah, A. -e.
    Shuhaib, Z. Al
    Alharis, R. A.
    Hussein, K. A.
    RUSSIAN JOURNAL OF GENERAL CHEMISTRY, 2024, 94 (03) : 719 - 728
  • [8] Ultrasound-assisted synthesis and anticancer evaluation of new pyrazole derivatives as cell cycle inhibitors
    Nitulescu, George Mihai
    Matei, Lilia
    Aldea, Ioana Madalina
    Draghici, Constantin
    Olaru, Octavian Tudorel
    Bleotu, Coralia
    ARABIAN JOURNAL OF CHEMISTRY, 2019, 12 (06) : 816 - 824
  • [9] Synthesis and Biological Evaluation of New Pyrazole-based Thiazolyl Hydrazone Derivatives as Potential Anticancer Agents
    Altintop, Mehlika Dilek
    Ozdemir, Ahmet
    Ilgin, Sinem
    Atli, Ozlem
    LETTERS IN DRUG DESIGN & DISCOVERY, 2014, 11 (07) : 833 - 839
  • [10] SYNTHESIS AND PHARMACOLOGICAL EVALUATION OF SOME NEW PYRAZOLE DERIVATIVES
    Nitulescu, George Mihai
    Paunescu, Horia
    Draghici, Constantin
    Missir, Alexandru-Vasile
    Coman, Oana Andreia
    Fulga, Ion
    FARMACIA, 2010, 58 (02) : 190 - 197
12345