Design, Synthesis, and Biological Evaluation of Some New N-(Substituted Pyridine-3-yl)-1,3,4-Oxadiazol-2-Amines

被引:0
作者
Patil, Priyanka A. [1 ,2 ]
Khulbe, Preeti [1 ]
Magdum, Chandrakant S. [3 ]
机构
[1] Suresh GyanVihar Univ, Sch Pharm, Dept Pharmaceut Chem, Jaipur, Rajasthan, India
[2] Dr Shivajirao Kadam Coll Pharm, Dept Pharmaceut Chem, Sangli, Maharashtra, India
[3] Rajarambapu Coll Pharm, Dept Pharmaceut Chem, Sangli, Maharashtra, India
关键词
MCF-7; Cytotoxicity; 1,3,4 Oxadiazole; HepG2; ANTICANCER; 1,3,4-OXADIAZOLE; DERIVATIVES; ANALOGS;
D O I
暂无
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
A series of some new oxadiazole derivatives was synthesized from substituted aryl isothiocyanates. All newly synthesized compounds were evaluated for in vitro cytotoxic activity on two standardized human cell lines, MCF 7 (breast cancer), and HepG2 (human liver cancer). Cytotoxicity was measured by MTT assay, the preliminary bioassay showed that most of the compounds had better antiproliferatory activity. Among the compounds evaluated, compound N-(4-methylphenyl)-5-(pyridin-3-yl)-1,3,4-oxadiazol-2-amine(3g) exhibited the significant cytotoxic property against MCF-7 (IC 50 = 29.25 )mu M) and compound N-(3-bromophenyl)-5-(pyridin-3-yl)-1,3,4-oxadiazol-2-amine (3j) exhibited the highest cytotoxic activity against HepG-2 tumor cell lines (IC 50 = 25.73 )mu M).
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页码:71 / 78
页数:8
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共 25 条
  • [1] Design, synthesis and in silico study of pyridine based 1,3,4-oxadiazole embedded hydrazinecarbothioamide derivatives as potent anti-tubercular agent
    Ambhore, Ajay N.
    Kamble, Sonali S.
    Kadam, Shuddhodan N.
    Kamble, Rahul D.
    Hebade, Madhav J.
    Hese, Shrikant V.
    Gaikwad, Milind V.
    Meshram, Rohan J.
    Gacche, Rajesh N.
    Dawane, Bhaskar S.
    [J]. COMPUTATIONAL BIOLOGY AND CHEMISTRY, 2019, 80 : 54 - 65
  • [2] Bala S., 2010, J. Pharm. Res, V3, P2993
  • [3] Raltegravir: The First HIV Integrase Inhibitor
    Cocohoba, Jennifer
    Dong, Betty J.
    [J]. CLINICAL THERAPEUTICS, 2008, 30 (10) : 1747 - 1765
  • [4] Dhiman AM, 2001, INDIAN J CHEM B, V40, P636
  • [5] Synthesis and screening of some novel substituted indoles contained 1,3,4-oxadiazole and 1,2,4-triazole moiety
    Gadegoni, Hemalatha
    Manda, Sarangapani
    [J]. CHINESE CHEMICAL LETTERS, 2013, 24 (02) : 127 - 130
  • [6] Harrison Michael R, 2009, Clin Adv Hematol Oncol, V7, P54
  • [7] ZIBOTENTAN Endothelin ETA Receptor Antagonist Oncolytic
    James, Nicholas D.
    Growcott, Jim W.
    [J]. DRUGS OF THE FUTURE, 2009, 34 (08) : 624 - 633
  • [8] Jwaid M, 2022, International Journal of Drug Delivery Technology, V12, P705, DOI [10.25258/ijddt.12.2.43, DOI 10.25258/IJDDT.12.2.43]
  • [9] Synthesis of novel 1,2,4-oxadiazoles and analogues as potential anticancer agents
    Kumar, Dalip
    Patel, Gautam
    Chavers, Angela K.
    Chang, Kuei-Hua
    Shah, Kavita
    [J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2011, 46 (07) : 3085 - 3092
  • [10] LigPlot+: Multiple Ligand-Protein Interaction Diagrams for Drug Discovery
    Laskowski, Roman A.
    Swindells, Mark B.
    [J]. JOURNAL OF CHEMICAL INFORMATION AND MODELING, 2011, 51 (10) : 2778 - 2786