Maxim Dragoun1, Thomas Günther2, Corazon Frias3, Albrecht Berkessel2, Aram Prokop3. 1. Department of Pediatric Hematology/Oncology, Children's Hospital Cologne, Amsterdamer Straße 59, 50735, Cologne, Germany. maximdragoun@gmail.com. 2. Department of Chemistry, Organic Chemistry, University of Cologne, Greinstraße 4, 50939, Cologne, Germany. 3. Department of Pediatric Hematology/Oncology, Children's Hospital Cologne, Amsterdamer Straße 59, 50735, Cologne, Germany.
Abstract
PURPOSE: We report on our preclinical findings of a simple salicylic diamine compound (THG 1213) which has yielded exceptional results as a potential chemotherapeutic drug. THG 1213 is an easy to synthesize chiral and metal-free salan compound. METHODS: THG 1213 was tested on several leukemia, lymphoma and solid tumor cell lines in vitro. The effects have been studied by LDH release essay, FACS flow cytometry, photometric cell count, immunoblotting, and NMR spectroscopy. RESULTS: THG 1213 selectively inhibits proliferation and induces apoptosis in leukemia, lymphoma and solid tumor cell lines. Necrosis or effects on healthy leucocytes could not be detected. Apoptosis is induced via the intrinsic and extrinsic pathways. The salan THG 1213 overcomes multidrug resistance in tumor cells and acts synergistically with vincristine and daunorubicin. CONCLUSIONS: THG 1213 displays remarkable antitumor properties. In particular, the lack of metallic components of THG 1213 could prove to be beneficial in future clinical trials, as metal-containing drugs are known to show severe side effects.
PURPOSE: We report on our preclinical findings of a simple salicylic diamine compound (THG 1213) which has yielded exceptional results as a potential chemotherapeutic drug. THG 1213 is an easy to synthesize chiral and metal-free salan compound. METHODS:THG 1213 was tested on several leukemia, lymphoma and solid tumor cell lines in vitro. The effects have been studied by LDH release essay, FACS flow cytometry, photometric cell count, immunoblotting, and NMR spectroscopy. RESULTS:THG 1213 selectively inhibits proliferation and induces apoptosis in leukemia, lymphoma and solid tumor cell lines. Necrosis or effects on healthy leucocytes could not be detected. Apoptosis is induced via the intrinsic and extrinsic pathways. The salan THG 1213 overcomes multidrug resistance in tumor cells and acts synergistically with vincristine and daunorubicin. CONCLUSIONS:THG 1213 displays remarkable antitumor properties. In particular, the lack of metallic components of THG 1213 could prove to be beneficial in future clinical trials, as metal-containing drugs are known to show severe side effects.
Entities:
Keywords:
Apoptosis; Cancer; Leukemia; Multidrug resistance; Salan
Authors: Elena B Rakhimova; Victor Yu Kirsanov; Elena V Tret'yakova; Leonard M Khalilov; Askhat G Ibragimov; Lilya U Dzhemileva; Vladimir A D'yakonov; Usein M Dzhemilev Journal: RSC Adv Date: 2020-06-04 Impact factor: 4.036
Authors: Sina M Hopff; Qifang Wang; Corazon Frias; Marie Ahrweiler; Nicola Wilke; Nathalie Wilke; Albrecht Berkessel; Aram Prokop Journal: J Cancer Res Clin Oncol Date: 2021-07-02 Impact factor: 4.553