2. Academic Validation
  3. Novel 3-(pyrazol-4-yl)-2-(1H-indole-3-carbonyl)acrylonitrile derivatives induce intrinsic and extrinsic apoptotic death mediated P53 in HCT116 colon carcinoma

Novel 3-(pyrazol-4-yl)-2-(1H-indole-3-carbonyl)acrylonitrile derivatives induce intrinsic and extrinsic apoptotic death mediated P53 in HCT116 colon carcinoma

  • Sci Rep. 2023 Dec 15;13(1):22486. doi: 10.1038/s41598-023-48494-7.
Magda F Mohamed 1 2,  Nada S Ibrahim 3,  Amna A Saddiq 4,  Ismail A Abdelhamid 5
Affiliations

Affiliations

  • 1 Department of Chemistry, College of Science and Arts at Khaulis, University of Jeddah, Jeddah, Saudi Arabia. magdafikry85@yahoo.com.
  • 2 Department of Chemistry (Biochemistry Branch), Faculty of Science, Cairo University, Giza, Egypt. magdafikry85@yahoo.com.
  • 3 Department of Chemistry (Biochemistry Branch), Faculty of Science, Cairo University, Giza, Egypt.
  • 4 Department of Biology, College of Science and Arts at Khaulis, University of Jeddah, Jeddah, Saudi Arabia.
  • 5 Chemistry Department, Faculty of Science, Cairo University, Giza, Egypt. ismail_shafy@cu.edu.eg.
PMID: 38110432 DOI: 10.1038/s41598-023-48494-7
Abstract

A novel series of α-cyano indolylchalcones was prepared, and their chemical structures were confirmed based on the different spectral data. Among them, compound 7f was observed to be the most effective bioactive chalcone with distinguished potency and selectivity against colorectal carcinoma (HCT116) with IC50 value (6.76 µg/mL) relative to the positive control (5 FU) (77.15 µg/mL). In a preliminary action study, the acrylonitrile chalcone 7f was found to enhance apoptotic action via different mechanisms like inhibition of some anti-apoptotic protein expression, regulation of some apoptotic proteins, production of caspases, and cell cycle arrest. All mechanisms suggested that compound 7f could act as a professional chemotherapeutic agent. Also, a molecular docking study was achieved on some selected proteins implicated in Cancer (Caspase 9, XIAP, P53 mutant Y220C, and MDM2) which showed variable interactions with compound 7f with good Gibbs free energy scores.

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