Trifluoromethyl Hydrolysis En Route to Corroles with Increased Druglikeness

Pinky Yadav, Sally Khoury, Natalia Fridman, Vinay K Sharma, Amit Kumar, Mahmoud Majdoub, Anil Kumar, Yael Diskin-Posner, Atif Mahammed*, Zeev Gross*

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

19 Citations (Scopus)

Abstract

Heme-like metal-chelating macrocycles, including expanded and contracted porphyrins, are of everlasting interest as drug candidates for numerous diseases. Still, all reported corrole derivatives (and most other heme analogues) do not fulfill the most basic standards expected for oral drug administration: a combination of low molecular weight and reasonable water solubility. We now disclose a very straightforward synthetic method that relies on surprisingly facile trifluoromethyl hydrolysis for gaining access to a new class of corroles that do satisfy all druglikeness criteria. The relevance is briefly exemplified for the iron corroles by demonstrating the ability to affect their association with plasma proteins and their performance for catalase-like decomposition of hydrogen peroxide.
Original languageEnglish
Pages (from-to)12829-12834
Number of pages6
JournalAngewandte Chemie - International Edition
Volume60
Issue number23
Early online date4 Apr 2021
DOIs
Publication statusPublished - 1 Jun 2021

Funding

This research was supported by the Israel Science Foundation (to Z.G.).

All Science Journal Classification (ASJC) codes

  • General Chemistry
  • Catalysis

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