Newly synthesized Olaparib Analogues: Estimation of The Clinical Activity Against MCF-7 breast Carcinoma Cell Line.

Document Type : Original Article

Authors

1 Mustansiriyah University, College of Science, Department of Chemistry, Baghdad-Iraq.

2 Mustansiriyah University, College of Pharmacy, Baghdad-Iraq.

Abstract

Abstract
Breast cancer is malignant tissue cells and has grown to be one of the world's most serious medical issues, as well as the cause of death in women. One of the most effective treatments for breast cancer is the use of poly (ADP-ribose) polymerase-1 (PARP) inhibitors. These two Olaparib analogs were tested on the Michigan Cancer Foundation-7 (MCF-7) and Madin Darby Canine Kidney (MDCK) cell lines in earlier unpublished work and found to be successful. One of these analogs, for example, is more active versus MCF-7 cell lines (IC50: 64.517 μg/mL versus 68.951 μg/mL for Olaparib) and has a better cytotoxic profile when tested on MDCK cell lines (IC50: 5.975 mg/mL versus 6.648 mg/mL for Olaparib). The obtained data concluded that two newly synthesized compounds had inhibitory activity against MCF-7, and they were close to the approved drug Olaparib. There is a good agreement between our docked results and the experimental results (In vitro study) of two compounds gave the high docking results that showed a promising cytotoxic activity among the tested compounds.

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History

  • Receive Date: 28 September 2021
  • Revise Date: 21 October 2021
  • Accept Date: 08 November 2021

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