Design, synthesis, anti-proliferative activity, and molecular docking studies of novel benzo[f]chromene, chromeno [2,3-d]pyrimidines and chromenotriazolo[1,5-c]pyrimidines
被引:14
作者:
Abu El-Azm, Fatma S. M.
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Ain Shams Univ, Fac Sci, Chem Dept, Khalifa El Maamon St,Abbasiya Sq, Cairo 11566, EgyptAin Shams Univ, Fac Sci, Chem Dept, Khalifa El Maamon St,Abbasiya Sq, Cairo 11566, Egypt
Abu El-Azm, Fatma S. M.
[1
]
El-Shahawi, Manal M.
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机构:
Ain Shams Univ, Fac Sci, Chem Dept, Khalifa El Maamon St,Abbasiya Sq, Cairo 11566, EgyptAin Shams Univ, Fac Sci, Chem Dept, Khalifa El Maamon St,Abbasiya Sq, Cairo 11566, Egypt
El-Shahawi, Manal M.
[1
]
Elgubbi, Amna S.
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机构:
Misurata Univ, Fac Sci, Chem Dept, Misurata, LibyaAin Shams Univ, Fac Sci, Chem Dept, Khalifa El Maamon St,Abbasiya Sq, Cairo 11566, Egypt
Elgubbi, Amna S.
[2
]
Madkour, Hassan M. F.
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Ain Shams Univ, Fac Sci, Chem Dept, Khalifa El Maamon St,Abbasiya Sq, Cairo 11566, EgyptAin Shams Univ, Fac Sci, Chem Dept, Khalifa El Maamon St,Abbasiya Sq, Cairo 11566, Egypt
Madkour, Hassan M. F.
[1
]
机构:
[1] Ain Shams Univ, Fac Sci, Chem Dept, Khalifa El Maamon St,Abbasiya Sq, Cairo 11566, Egypt
[2] Misurata Univ, Fac Sci, Chem Dept, Misurata, Libya
In seeking to establish new anticancer agents, a group of novel substituted chromeno[2,3-d]pyrimidine and chromenotriazolo[1,5-c]pyrimidine derivatives were designed and synthesized as potential anti-proliferative agents. Chromeno[2,3-d]pyrimidine derivatives were prepared via reaction of ethyl formimidate derivative 2 with different nitrogen nucleophiles and chromenotriazolo[1,5-c]pyrimidine derivatives were obtained from treatment of cyanomethyl derivative 14 with various electrophilic reagents. The structures of the synthesized compounds were substantiated on the basis of spectral data and elemental analysis. All the synthesized products were evaluated for their antiproliferative activity against two human tumor cell lines; breast adenocarcinoma (MCF-7) and hepatocellular carcinoma (HepG-2) in addition to normal fibroblasts (WI-38). Derivatives 8 and 21 had significant and selective anti-proliferative activity against liver and breast cell lines without harming the normal fibroblasts. The molecular docking studies of most active compounds 8, 10, and 21 were performed to examine their binding pattern with protein receptors (PDB: 1SA0).
机构:
Natl Res Ctr, Appl Organ Chem Dept, Giza 12622, Egypt
Natl Res Ctr, Ctr Excellence Adv Sci, Giza 12622, EgyptNatl Res Ctr, Appl Organ Chem Dept, Giza 12622, Egypt
Ali, Korany A.
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Hafez, Naglaa A. Abdel
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Natl Res Ctr, Appl Organ Chem Dept, Giza 12622, EgyptNatl Res Ctr, Appl Organ Chem Dept, Giza 12622, Egypt
Hafez, Naglaa A. Abdel
;
Elsayed, Mohamed A.
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Natl Res Ctr, Appl Organ Chem Dept, Giza 12622, EgyptNatl Res Ctr, Appl Organ Chem Dept, Giza 12622, Egypt
Elsayed, Mohamed A.
;
El-Shahawi, Manal M.
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机构:
Ain Shams Univ, Fac Sci, Chem Dept, Cairo, EgyptNatl Res Ctr, Appl Organ Chem Dept, Giza 12622, Egypt
El-Shahawi, Manal M.
;
El-Hallouty, Salwa M.
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机构:
Natl Res Ctr, Dept Pharmacognosy, Pharmaceut & Drug Ind Div, Drug Bioassay Cell Culture Lab, Giza 12622, EgyptNatl Res Ctr, Appl Organ Chem Dept, Giza 12622, Egypt
El-Hallouty, Salwa M.
;
Amr, Abd El-Galil E.
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机构:
Natl Res Ctr, Appl Organ Chem Dept, Giza 12622, Egypt
King Saud Univ, Coll Pharm, Dept Pharmaceut Chem, DEDC, Riyadh, Saudi ArabiaNatl Res Ctr, Appl Organ Chem Dept, Giza 12622, Egypt
机构:
ROYAL MELBOURNE HOSP,WALTER & ELIZA HALL INST MED RES,PARKVILLE,VIC 3050,AUSTRALIAROYAL MELBOURNE HOSP,WALTER & ELIZA HALL INST MED RES,PARKVILLE,VIC 3050,AUSTRALIA
DENIZOT, F
;
LANG, R
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机构:
ROYAL MELBOURNE HOSP,WALTER & ELIZA HALL INST MED RES,PARKVILLE,VIC 3050,AUSTRALIAROYAL MELBOURNE HOSP,WALTER & ELIZA HALL INST MED RES,PARKVILLE,VIC 3050,AUSTRALIA
机构:
Natl Res Ctr, Appl Organ Chem Dept, Giza 12622, Egypt
Natl Res Ctr, Ctr Excellence Adv Sci, Giza 12622, EgyptNatl Res Ctr, Appl Organ Chem Dept, Giza 12622, Egypt
Ali, Korany A.
;
Hafez, Naglaa A. Abdel
论文数: 0引用数: 0
h-index: 0
机构:
Natl Res Ctr, Appl Organ Chem Dept, Giza 12622, EgyptNatl Res Ctr, Appl Organ Chem Dept, Giza 12622, Egypt
Hafez, Naglaa A. Abdel
;
Elsayed, Mohamed A.
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h-index: 0
机构:
Natl Res Ctr, Appl Organ Chem Dept, Giza 12622, EgyptNatl Res Ctr, Appl Organ Chem Dept, Giza 12622, Egypt
Elsayed, Mohamed A.
;
El-Shahawi, Manal M.
论文数: 0引用数: 0
h-index: 0
机构:
Ain Shams Univ, Fac Sci, Chem Dept, Cairo, EgyptNatl Res Ctr, Appl Organ Chem Dept, Giza 12622, Egypt
El-Shahawi, Manal M.
;
El-Hallouty, Salwa M.
论文数: 0引用数: 0
h-index: 0
机构:
Natl Res Ctr, Dept Pharmacognosy, Pharmaceut & Drug Ind Div, Drug Bioassay Cell Culture Lab, Giza 12622, EgyptNatl Res Ctr, Appl Organ Chem Dept, Giza 12622, Egypt
El-Hallouty, Salwa M.
;
Amr, Abd El-Galil E.
论文数: 0引用数: 0
h-index: 0
机构:
Natl Res Ctr, Appl Organ Chem Dept, Giza 12622, Egypt
King Saud Univ, Coll Pharm, Dept Pharmaceut Chem, DEDC, Riyadh, Saudi ArabiaNatl Res Ctr, Appl Organ Chem Dept, Giza 12622, Egypt
机构:
ROYAL MELBOURNE HOSP,WALTER & ELIZA HALL INST MED RES,PARKVILLE,VIC 3050,AUSTRALIAROYAL MELBOURNE HOSP,WALTER & ELIZA HALL INST MED RES,PARKVILLE,VIC 3050,AUSTRALIA
DENIZOT, F
;
LANG, R
论文数: 0引用数: 0
h-index: 0
机构:
ROYAL MELBOURNE HOSP,WALTER & ELIZA HALL INST MED RES,PARKVILLE,VIC 3050,AUSTRALIAROYAL MELBOURNE HOSP,WALTER & ELIZA HALL INST MED RES,PARKVILLE,VIC 3050,AUSTRALIA