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Journal Article Ppublish 2 citations

PubMed: 38708686 DOI: 10.4155/fmc-2023-0375

Synthesis and antiproliferative evaluation of novel 3,5,8-trisubstituted coumarins against breast cancer.

Future Med Chem 16(11):1053-1073

Authors: Manar G Salem, Alaa M Alqahtani, Suraj N Mali, Hussah Abdullah Alshwyeh, Rahul D Jawarkar, Abdulmalik S Altamimi, Samar Z Alshawwa, Ebtesam Al-Olayan, Essa M Saied, Mohamed F Youssef

Affiliations

  • Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Suez Canal University, Ismailia, 41522, Egypt.
  • Department of Pharmaceutical Sciences, Faculty of Pharmacy, Umm Al-Qura University, Makkah, 21955, Saudi Arabia.
  • School of Pharmacy, DY Patil Deemed to be University Sector 7, Nerul, Navi Mumbai, 400706, India.
  • Department of Biology, College of Science, Imam Abdulrahman Bin Faisal University, Dammam, 31441, Saudi Arabia.
  • Basic & Applied Scientific Research Centre, Imam Abdulrahman Bin Faisal University, PO Box 1982, Dammam, 31441, Saudi Arabia.
  • Department of Medicinal Chemistry & Drug Discovery, Dr. Rajendra Gode Institute of Pharmacy, University Mardi Road, Amravati, 444603, India.
  • Department of Pharmaceutical Chemistry, College of Pharmacy, Prince Sattam Bin Abdulaziz University, PO Box 173, Alkharj, 11942, Saudi Arabia.
  • Department of Pharmaceutical Sciences, College of Pharmacy, Princess Nourah bint Abdulrahman University, PO Box 84428, Riyadh, 11671, Saudi Arabia.
  • Department of Zoology, College of Science, King Saud University, Riyadh, 11451, Saudi Arabia.
  • Chemistry Department (Biochemistry Division), Faculty of Science, Suez Canal University, Ismailia, 41522, Egypt.
  • Institute for Chemistry, Humboldt Universität zu Berlin, Brook-Taylor-Str. 2, Berlin, 12489, Germany.
  • Chemistry Department (Organic Chemistry Division), Faculty of Science, Suez Canal University, Ismailia, 41522, Egypt.

Abstract

This study focused on designing and synthesizing novel derivatives of 3,5,8-trisubstituted coumarin. The synthesized compounds, particularly compound , exhibited significant cytotoxic effects on MCF-7 cells, surpassing staurosporine, and reduced toxicity toward MCF-10A cells, highlighting potential pharmacological advantages. Further, compound altered the cell cycle and significantly increased apoptosis in MCF-7 cells, involving both early (41.7-fold) and late stages (33-fold), while moderately affecting necrotic signaling. The antitumor activity was linked to a notable reduction (4.78-fold) in topoisomerase IIβ expression. Molecular modeling indicated compound 's strong affinity for EGFR, human EGF2 and topoisomerase II proteins. These findings highlight compound as a multifaceted antitumor agent for breast cancer.

MeSH

Coumarins, Breast Neoplasms, Chemistry, Pharmaceutical, Mcf-7 Cells

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