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Amide Coupling Reaction for the Synthesis of Bispyridine-based Ligands and Their Complexation to Platinum as Dinuclear Anticancer Agents
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Unsymmetrical Pd(II) Pincer Complexes with Benzothiazole and Thiocarbamate Flanking Units: Expedient Solvent-Free

Vladimir A Kozlov1, Diana V Aleksanyan1,2, Svetlana G Churusova1

  • 1A. N. Nesmeyanov Institute of Organoelement Compounds, Russian Academy of Sciences, ul. Vavilova 28, Str. 1, 119334 Moscow, Russia.

International Journal of Molecular Sciences
|December 23, 2023
PubMed

Insights

New palladium(II) pincer complexes show potent anticancer activity against diverse cancer cell lines. These novel compounds, synthesized using an efficient solid-phase strategy, offer promising therapeutic potential for cancer treatment.

Area of Science:

  • Medicinal Chemistry
  • Organometallic Chemistry
  • Cancer Research

Background:

  • Cancer remains a significant global health threat, driving the search for novel chemotherapeutic agents.
  • Transition metal complexes are central to developing new anticancer drugs.
  • Ligand design is crucial for optimizing the anticancer efficacy of metal complexes.

Purpose of the Study:

  • To synthesize novel unsymmetrical pincer ligands combining benzothiazole and thiocarbamate donor groups.
  • To prepare S,C,N-type Pd(II) pincer complexes via direct cyclopalladation.
  • To evaluate the anticancer cytotoxicity and apoptosis-inducing potential of the synthesized palladacycles.

Main Methods:

  • Synthesis of unsymmetrical pincer ligands.
  • Direct cyclopalladation for Pd(II) complex formation (solution and solvent-free).
  • Characterization using NMR, IR, and X-ray diffraction (single-crystal and powder).
  • Cytotoxicity assays against multiple solid and blood cancer cell lines.
  • Apoptosis induction studies in drug-sensitive and drug-resistant leukemia cells.

Main Results:

  • Efficient synthesis of S,C,N-type Pd(II) pincer complexes was achieved using a solid-phase strategy.
  • The synthesized palladacycles demonstrated significant cytotoxicity against human colorectal carcinoma (HCT116), breast cancer (MCF7), prostate adenocarcinoma (PC3), chronic myelogenous leukemia (K562), multiple plasmacytoma (AMO1), and acute lymphoblastic leukemia (H9) cell lines.
  • A dimethylamino-substituted derivative showed particularly high efficacy and induced apoptosis in both parental and doxorubicin-resistant K562 cells.

Conclusions:

  • Unsymmetrical pincer ligands enable the efficient synthesis of novel Pd(II) complexes with potent anticancer properties.
  • The developed palladacycles exhibit broad-spectrum cytotoxicity and overcome drug resistance, highlighting their therapeutic potential.
  • This research validates the anticancer promise of S,C,N-type palladacycles for future drug development.
Keywords:
benzothiazolescytotoxicitypalladiumpincer complexessolid-phase synthesisthiocarbamates

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