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).
引用
收藏
页码:71 / 78
页数:8
相关论文
共 50 条
  • [1] Synthesis Antioxidant and Antimicrobial Activities of N-[(5′-Substituted 2′-phenyl-1H-indol-3′-yl)methylene]-5-(pyridin-4-yl)-1,3,4-oxadiazol-2-amines
    Saundane, A. R.
    Katkar, Vijaykumar
    Vaijinath, A. Verma
    JOURNAL OF CHEMISTRY, 2013, 2013
  • [2] Substituted N-(thieno[2,3-b]pyridine-3-yl)acetamides: synthesis, reactions, and biological activity
    Victor V. Dotsenko
    Dmitrii S. Buryi
    Darya Yu. Lukina
    Angelica N. Stolyarova
    Nicolai A. Aksenov
    Inna V. Aksenova
    Vladimir D. Strelkov
    Lyudmila V. Dyadyuchenko
    Monatshefte für Chemie - Chemical Monthly, 2019, 150 : 1973 - 1985
  • [3] Synthesis and Biological Potentials of 5-aryl-N-[4-(trifluoromethyl) phenyl]-1,3,4-oxadiazol-2-amines
    Ahsan, Mohamed Jawed
    Hassan, Mohd. Zaheen
    Jadav, Surender Singh
    Geesi, Mohammed H.
    Bakht, Mohammed Afroz
    Riadi, Yassine
    Salahuddin
    Akhtar, Md. Sayeed
    Mallick, Mohammad Nasar
    Akhter, Md. Habban
    LETTERS IN ORGANIC CHEMISTRY, 2020, 17 (02) : 133 - 140
  • [4] Substituted N-(thieno[2,3-b]pyridine-3-yl)acetamides: synthesis, reactions, and biological activity
    Dotsenko, Victor V.
    Buryi, Dmitrii S.
    Lukina, Darya Yu
    Stolyarova, Angelica N.
    Aksenov, Nicolai A.
    Aksenova, Inna, V
    Strelkov, Vladimir D.
    Dyadyuchenko, Lyudmila, V
    MONATSHEFTE FUR CHEMIE, 2019, 150 (11): : 1973 - 1985
  • [5] Synthesis and evaluation of 5-(1H-indo1-3-yl)-N-aryl-1,3,4-oxadiazol-2-amines as Bcl-2 inhibitory anticancer agents
    Hamdy, Rania
    Ziedan, Noha I.
    Ali, Samia
    Bordoni, Cinzia
    El-Sadek, Mohamed
    Lashin, Elsaid
    Brancale, Andrea
    Jones, Arwyn T.
    Westwell, Andrew D.
    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2017, 27 (04) : 1037 - 1040
  • [6] Synthesis, Antiproliferative, and Antioxidant Activities of Substituted N-[(1,3,4-Oxadiazol-2-yl) Methyl] Benzamines
    Ahsan, Mohamed Jawed
    Bhandari, Lakshya
    Makkar, Shally
    Singh, Rajan
    Hassan, Mohd Zaheen
    Geesi, Mohammed H.
    Bakht, Mohamed Afroz
    Jadav, Surender Singh
    Balaraju, Tuniki
    Riadi, Yassine
    Rani, Sandhya
    Khalilullah, Habibullah
    Gorantla, Vasubabu
    Hussain, Afzal
    LETTERS IN DRUG DESIGN & DISCOVERY, 2020, 17 (02) : 145 - 154
  • [7] Synthesis and In-Vitro Antimycobacterial Evaluation of N-Arylidene-5-Aryl-1,3,4-Oxadiazol-2-Amines Derivatives
    Mazen Almehmadi
    Osama Abdulaziz
    Mamdouh Allahyani
    Abdullah Y. A. Alzahrani
    Kamal Kant Joshi
    Mohammad Asif
    Pharmaceutical Chemistry Journal, 2025, 58 (12) : 1846 - 1850
  • [8] Synthesis and Antimicrobial Activity of New Substituted 5-(Pyridine-3-yl)-1,3,4-Thiadiazoles and Their Sugar Derivatives
    El-Sayed, Wael A.
    Metwally, Mohamed A.
    Nada, Doaa S.
    Mohamed, Asem A.
    Abdel-Rahman, Adel A. -H.
    JOURNAL OF HETEROCYCLIC CHEMISTRY, 2013, 50 (02) : 194 - 201
  • [9] Ultrasound-Assisted Synthesis, Antioxidant Activity and Computational Study of 1,3,4-Oxadiazol-2-amines
    Beyzaei, Hamid
    Sargazi, Soheila
    Bagherzade, Ghodsieh
    Moradi, Ashraf
    Yarmohammadi, Elahe
    ACTA CHIMICA SLOVENICA, 2021, 68 (01) : 109 - 117
  • [10] SYNTHESIS AND BIOLOGICAL PROPERTIES OF SOME BASIC N-(5-ARYL-1,3,4-OXADIAZOL-2-YL) PROPANAMIDES AND BUTANAMIDES
    SAXENA, VK
    SINGH, AR
    AGARWAL, RK
    MEHRA, SC
    JOURNAL OF THE INDIAN CHEMICAL SOCIETY, 1983, 60 (06) : 575 - 577