SR141716A;
NVP-AUY922;
Pyrazole;
Isoxazole and anticancer activity;
D O I:
10.1016/j.cdc.2022.100938
中图分类号:
O6 [化学];
学科分类号:
0703 ;
摘要:
A novel library of isoxazole bearing N-arylpyrazole (12a -j) derivatives has been designed synthesized and their structures were confirmed by 1HNMR, 13CNMR and mass spectral analysis. Further, these compounds were evaluated for their anticancer activity towards four human cancer cell line including MCF-7: human breast, A549: human lung, DU -145: human prostrate and MDA MB -231: human breast) and etoposide used standard drug. Most of the synthesized compounds showed good to moderate activity. Among them, these compounds 12b, 12c, 12d, 12f, 12g and 12h displayed more potent than etoposide. Particularly, compound 12h has showed most promising activity compare to all compounds (MCF-7 = 0.31 +/- 0.044 mu M, A549 = 0.47 +/- 0.059 mu M, Du -145 = 0.19 +/- 0.053 mu M and MDA MB -231 = 0.37 +/- 0.098 mu M)
机构:
Imam Mohammad Ibn Saud Islamic Univ IMSIU, Fac Sci, Dept Chem, POB 90950, Riyadh 11623, Saudi Arabia
Natl Res Ctr, Photochem Dept, Heterocycl & Nucleosides Unit, Cairo, EgyptImam Mohammad Ibn Saud Islamic Univ IMSIU, Fac Sci, Dept Chem, POB 90950, Riyadh 11623, Saudi Arabia
Hafez, Hend N.
El-Gazzar, Abdel-Rahman B. A.
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机构:
Imam Mohammad Ibn Saud Islamic Univ IMSIU, Fac Sci, Dept Chem, POB 90950, Riyadh 11623, Saudi Arabia
Natl Res Ctr, Photochem Dept, Heterocycl & Nucleosides Unit, Cairo, EgyptImam Mohammad Ibn Saud Islamic Univ IMSIU, Fac Sci, Dept Chem, POB 90950, Riyadh 11623, Saudi Arabia
机构:
Alexandru Ioan Cuza Univ, Fac Chem, Dept Organ Chem, Iasi 700506, RomaniaAlexandru Ioan Cuza Univ, Fac Chem, Dept Organ Chem, Iasi 700506, Romania
Baciu-Atudosie, Lavinia
Ghinet, Alina
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Alexandru Ioan Cuza Univ, Fac Chem, Dept Organ Chem, Iasi 700506, Romania
Univ Lille Nord France, F-59000 Lille, France
UCLille, HEI, Lab Pharmacochim, EA GRIIOT 4481, F-59046 Lille, FranceAlexandru Ioan Cuza Univ, Fac Chem, Dept Organ Chem, Iasi 700506, Romania
Ghinet, Alina
Farce, Amaury
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Univ Lille Nord France, F-59000 Lille, France
Inst Chim Pharmaceut Albert Lespagnol, EA GRIIOT 4481, IFR114, F-59006 Lille, FranceAlexandru Ioan Cuza Univ, Fac Chem, Dept Organ Chem, Iasi 700506, Romania
Farce, Amaury
Dubois, Joelle
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Inst Chim Subst Nat, Ctr Rech Gif, CNRS UPR2301, F-91198 Gif Sur Yvette, FranceAlexandru Ioan Cuza Univ, Fac Chem, Dept Organ Chem, Iasi 700506, Romania
Dubois, Joelle
Belei, Dalila
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Alexandru Ioan Cuza Univ, Fac Chem, Dept Organ Chem, Iasi 700506, RomaniaAlexandru Ioan Cuza Univ, Fac Chem, Dept Organ Chem, Iasi 700506, Romania
Belei, Dalila
Bicu, Elena
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Alexandru Ioan Cuza Univ, Fac Chem, Dept Organ Chem, Iasi 700506, RomaniaAlexandru Ioan Cuza Univ, Fac Chem, Dept Organ Chem, Iasi 700506, Romania