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Development, synthesis and validation of improved c-Myc/Max inhibitors.
Yildirim, Sümbül; Kocabas, Fatih; Mermer, Arif.
  • Yildirim S; Department of Genetics and Bioengineering, Faculty of Engineering, Yeditepe University, Istanbul, Turkey.
  • Kocabas F; Graduate School of Natural and Applied Sciences, Yeditepe University, Istanbul, Turkey.
  • Mermer A; Institute for Diabetes and Cancer, Helmholtz Diabetes Center, Helmholtz Center, Neuherberg, Germany.
J Cell Mol Med ; 28(8): e18272, 2024 Apr.
Article en En | MEDLINE | ID: mdl-38568057
ABSTRACT
The pathophysiological foundations of various diseases are often subject to alteration through the utilization of small compounds, rendering them invaluable tools for the exploration and advancement of novel therapeutic strategies. Within the scope of this study, we meticulously curated a diverse library of novel small compounds meticulously designed to specifically target the c-Myc/Max complex. We conducted in vitro examinations of novel c-Myc inhibitors across a spectrum of cancer cell lines, including PANC1 (pancreatic adenocarcinoma), MCF7 (breast carcinoma), DU-145 (prostate carcinoma), and A549 (lung cancer). The initial analysis involved a 25 µM dose, which enabled the identification of potent anticancer compounds effective against a variety of tumour types. We identified c-Myc inhibitors with remarkable potency, featuring IC50 values as low as 1.6 µM and up to 40 times more effective than the reference molecule in diminishing cancer cell viability. Notably, c-Myc-i7 exhibited exceptional selectivity, displaying 37-fold and 59-fold preference for targeting prostate and breast cancers, respectively, over healthy cells. Additionally, we constructed drug-likeness models. This study underscores the potential for in vitro investigations of various tumour types using novel c-Myc inhibitors to yield ground-breaking and efficacious anticancer compounds.
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Texto completo: 1 Banco de datos: MEDLINE Asunto principal: Neoplasias Pancreáticas / Adenocarcinoma Límite: Humans / Male Idioma: En Año: 2024 Tipo del documento: Article

Texto completo: 1 Banco de datos: MEDLINE Asunto principal: Neoplasias Pancreáticas / Adenocarcinoma Límite: Humans / Male Idioma: En Año: 2024 Tipo del documento: Article