SYNTHESIS, CYTOTOXIC EVALUATION AND MOLECULAR DOCKING STUDIES OF NEW 3-(1,3,4-OXADIAZOLYL)-QUINOLINONE DERIVATIVES AGAINST BREAST CANCER CELL LINES
By: Muthadi, S
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Contributor(s): Guda, R.
Publisher: Mumbai Indian Drug Manufacture's Association - IDMA 2018Edition: Vol. 55 (11) November.Description: 19-31p.Subject(s): PHARMACEUTICS | Flavones Azaflavones Aromatase Inhibitors
In:
Baghel, D. S. AMALGAMATION OF AYURVEDIC CONCEPT WITH MODERN MEDICAL PRACTICE TO MANAGE KIDNEY STONE DISEASE (UROLITHIASIS)Summary: A series of new substituted 3-(5-substituted-1,3,4-oxadiazol-2-yl)-4(1H)-quinolinone derivatives (5a-t) have been designed and synthesized using appropriate protocols. All of them were screened for cytotoxic activity against human breast cancer cell lines (MCF-7 and T47D) and antioxidant activity (DPPH method). Among them, 5f exhibited promising inhibitory activity with IC50 values 7.429 and 8.388 against the two cell lines chosen. The molecular interactions with target (aromatase receptor by docking) were found to correlate well with in vitro cytotoxic activity, i.e. 5f showed the high binding affinity -12.34 kcal/ mol. In the antioxidant screening also, 5f and 5h were found superior to others.
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School of Pharmacy Archieval Section | Not for loan | 2018313 |
A series of new substituted 3-(5-substituted-1,3,4-oxadiazol-2-yl)-4(1H)-quinolinone derivatives (5a-t) have been designed and synthesized using appropriate protocols. All of them were screened for cytotoxic activity against human breast cancer cell lines (MCF-7 and T47D) and antioxidant activity (DPPH method). Among them, 5f exhibited promising inhibitory activity with IC50 values 7.429 and 8.388 against the two cell lines chosen. The molecular interactions with target (aromatase receptor by docking) were found to correlate well with in vitro cytotoxic activity, i.e. 5f showed the high binding affinity -12.34 kcal/ mol. In the antioxidant screening also, 5f and 5h were found superior to others.
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