Design and synthesis of pyrimidine molecules endowed with thiazolidin-4-one as new anticancer agents

被引:37
|
作者
Rashid, Mohd [1 ]
Husain, Asif [1 ]
Shaharyar, Mohammad [1 ]
Mishra, Ravinesh [1 ]
Hussain, Afzal [1 ]
Afzal, Obaid [1 ]
机构
[1] Jamie Hamdard Hamdard Univ, Dept Pharmaceut Chem, Fac Pharm, New Delhi 110062, India
关键词
In-vitro anticancer activity; NCI 60 cell line; CDK; 2; enzyme; Thiazolidin-4-one; NATIONAL-CANCER-INSTITUTE; CYCLIN-DEPENDENT KINASES; TRIAZOLO-THIADIAZOLES; BEARING OXADIAZOLE; DRUG DISCOVERY; DERIVATIVES; INHIBITORS; ANTIBACTERIAL; CHEMOTHERAPY; OLOMOUCINE;
D O I
10.1016/j.ejmech.2014.06.033
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Design and synthesis of new pyrimidine derivatives clubbed with thiazolidin-4-one from 4-(2-chlorophenyl)-6-(2,4-dichlorophenyl)pyrimidin-2-amine and their in vitro anticancer activities were screened at National Cancer Institute (NCI), USA against full NCI 60 cell lines. Compound 2 (NSC: 765735) exhibited remarkable growth inhibition at single dose (10 mu M) and encourage chosen for broadcast at 10-fold dilutions of five different concentrations (0.01, 0.1, 1, 10 and 100 mu M). The compound 2 was found better quality for Lung cancer cell line (HOP-92) by viewing growth inhibition (GI(50) 0.52) and no cytotoxicity seen (LC50 > 100). Molecular docking study was performed using Maestro 9.0 (Schrodinger Inc. USA) to provide binding mode into binding sites of CDK2. Compound 2 could be used as a lead compound for developing new potential anticancer agents. (C) 2014 Elsevier Masson SAS. All rights reserved.
引用
收藏
页码:630 / 645
页数:16
相关论文
共 50 条
  • [41] Thiazolidin-4-one and thiazinan-4-one derivatives analogous to rosiglitazone as potential antihyperglycemic and antidyslipidemic agents
    Raza, Saman
    Srivastava, Swayam P.
    Srivastava, Daya S.
    Srivastava, Arvind K.
    Haq, W.
    Katti, S. B.
    EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2013, 63 : 611 - 620
  • [42] An expedient synthesis of new 2-(furoxan-3-yl)thiazolidin-4-one derivatives
    Kumar, Singam Naveen
    Kumar, Chebolu Naga Sesha Sai Pavan
    Anudeep, Sri Ranga Vanarasi
    Sharma, Kirti Kumari
    Rao, Vaidya Jayathirtha
    Babu, Nanubolu Jagadeesh
    ARKIVOC, 2016, : 32 - 49
  • [43] An efficient synthesis of substituted thiazolidin-4-one derivatives via pyrazole carbothiamides
    Behzadi, Masoomeh
    Saidi, Kazem
    Khabazzadeh, Hojatollah
    RESEARCH ON CHEMICAL INTERMEDIATES, 2015, 41 (04) : 1873 - 1880
  • [44] Synthesis of some 5-arylidene-2-(4-acetamidophenylimino)-thiazolidin-4-one derivatives and exploring their breast anticancer activity
    Abumelha, Hana M. A.
    Saeed, Ali
    JOURNAL OF HETEROCYCLIC CHEMISTRY, 2020, 57 (04) : 1816 - 1824
  • [45] Recent advances in synthetic strategies and SAR of thiazolidin-4-one containing molecules in cancer therapeutics
    Archana Sharma
    Diksha Sharma
    Neha Saini
    Sunil V. Sharma
    Vijay Kumar Thakur
    Ramesh K. Goyal
    Prabodh Chander Sharma
    Cancer and Metastasis Reviews, 2023, 42 : 847 - 889
  • [46] Recent advances in synthetic strategies and SAR of thiazolidin-4-one containing molecules in cancer therapeutics
    Sharma, Archana
    Sharma, Diksha
    Saini, Neha
    Sharma, Sunil V.
    Thakur, Vijay Kumar
    Goyal, Ramesh K.
    Sharma, Prabodh Chander
    CANCER AND METASTASIS REVIEWS, 2023, 42 (03) : 847 - 889
  • [47] Structure and temperature controlled synthesis of novel thiazolidin-4-one derivatives bearing an azasugar
    Chen, Hua
    Wei, Sinan
    Zhang, Hongbo
    Li, Xiaoliu
    TETRAHEDRON-ASYMMETRY, 2013, 24 (08) : 457 - 463
  • [48] Synthesis and Proliferative Effects on T Lymphocytes of Novel Thiazolidin-4-one Linked Pseudotrisaccharides
    Chen, Hua
    Gao, Fang
    Yin, Qingmei
    Li, Chunxiao
    Li, Na
    Meng, Ming
    Li, Xiaoliu
    CHINESE JOURNAL OF ORGANIC CHEMISTRY, 2012, 32 (05) : 943 - 948
  • [49] SYNTHESIS, CHARACTERIZATION, AND BIOLOGICAL SCREENING OF SOME NOVEL THIAZOLIDIN-4-ONE AND α-AMINOPHOSPHONATE DERIVATIVES
    Badadhe, P. V.
    Chavan, N. M.
    Ghotekar, D. S.
    Mandhane, P. G.
    Joshi, R. S.
    Gill, C. H.
    PHOSPHORUS SULFUR AND SILICON AND THE RELATED ELEMENTS, 2011, 186 (10) : 2021 - 2032
  • [50] Synthesis and Tyrosinase Inhibitory Activity of Novel Benzimidazole/Thiazolidin-4-one Hybrid Derivatives
    Khraisat, Leen Mohammad Amin Farhan
    Sabuncuoglu, Suna
    Girgin, Gozde
    Tan, Oya Unsal
    CHEMISTRY & BIODIVERSITY, 2024, 21 (02)