| 000 | 02665cam a2200337 a 4500 | ||
|---|---|---|---|
| 003 | EG-GiCUC | ||
| 005 | 20250223032519.0 | ||
| 008 | 200203s2020 ua h f m 000 0 eng d | ||
| 040 |
_aEG-GiCUC _beng _cEG-GiCUC |
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| 041 | 0 | _aeng | |
| 049 | _aDeposite | ||
| 097 | _aPh.D | ||
| 099 | _aCai01.08.05.Ph.D.2020.Ma.N | ||
| 100 | 0 | _aMai Saeed Mohamed Nour | |
| 245 | 1 | 0 |
_aNew oxadiazole based molecules : _bDesign, synthesis, molecular modeling and biological screening / _cMai Saeed Mohamed Nour ; Supervised Nehad Abul Magd Elsayed , Reem Khidr Arafa |
| 246 | 1 | 5 |
_aمركبات مستحدثة مستندة على الاوكسادياذول : _bتصميم: تشييد: النمذجة الجزيئية والمسح البيولوجى |
| 260 |
_aCairo : _bMai Saeed Mohamed Nour , _c2020 |
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| 300 |
_a114 P. : _bfacsimiles ; _c25cm |
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| 502 | _aThesis (Ph.D.) - Cairo University - Faculty of Pharmacy - Department of Pharmaceutical Chemistry | ||
| 520 | _aNovel heterocyclic oxadiazoles viz. 2-subsituted-5-(4-pyridyl)-1,3,4-oxadiazoles, 2-subsituted-5-(3-pyridyl)-1,3,4-oxadiazoles and 2-subsituted-5-(phenyl/4-chlorophenyl-1,3,4-oxadiazoles) were designed and synthesized as potential anticancer agents. In this investigation, all compounds were evaluated for their COX-1 and COX-2 inhibitory activity in vitro as new therapeutic approaches highlighted observations of cytotoxic effects associated with selective COX-2 inhibition. Results showed that most of the derivatives demonstrated inhibition towards both isoforms of COX with higher selectivity towards COX-2. Some derivatives were more potent than the standard reference drugs indomethacin, diclofenac sodium and celecoxib. Then, nine selected compounds (IIId, VIb, VIIc, IX, XI, XIIa, XIVa, XVIb and XVIIIb) were subjected to cytotoxic screening against UO-31 renal cancer cell line using MTT assay. Compounds IIId, IX and XIIa displayed promising behavior by showing good anticancer activity. Moreover, kinase inhibitory assay against the tyrosine kinase EGFR was performed for the three compounds showing the highest cytotoxic activity. The tested compounds were potent against EGFR with the highest activity being observed for compound IX showing nearly double the potency of the reference drug Erlotinib | ||
| 530 | _aIssued also as CD | ||
| 653 | 4 | _aAdenosine triphosphate (ATP) | |
| 653 | 4 | _aAngstrom (Å) | |
| 653 | 4 | _aProtein kinase B (Akt) | |
| 700 | 0 |
_aNehad Abulmagd Elsayed , _eSupervisor |
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| 700 | 0 |
_aReem Khidr Arafa , _eSupervisor |
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| 856 | _uhttp://172.23.153.220/th.pdf | ||
| 905 |
_aNazla _eRevisor |
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| 905 |
_aShimaa _eCataloger |
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| 942 |
_2ddc _cTH |
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| 999 |
_c76498 _d76498 |
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