2H-1,2,3-Triazole-chalcones as novel cytotoxic agents against prostate cancer
| Autor: | Carlos M.D. Silva Junior, Laiza B. Loureiro, Karin J.P. Rocha-Brito, Sandro J. Greco, Sergio Pinheiro, Estela M.F. Muri, Karina M. Rotamiro, Rodolfo G. Fiorot, Eclair Venturini Filho, Maria Clara R. Freitas, Anderson R.A. Guimarães, Erick M.C. Pinheiro, José Walkimar de M. Carneiro, Jaqueline C. Pessôa |
|---|---|
| Rok vydání: | 2020 |
| Předmět: |
Male
Chalcone 1 2 3-Triazole Clinical Biochemistry Cell Quantitative Structure-Activity Relationship Pharmaceutical Science Antineoplastic Agents 01 natural sciences Biochemistry chemistry.chemical_compound Prostate cancer Chalcones Drug Discovery medicine Humans Viability assay Cytotoxicity Molecular Biology IC50 Molecular Structure 010405 organic chemistry Organic Chemistry Prostatic Neoplasms Triazoles medicine.disease In vitro 0104 chemical sciences 010404 medicinal & biomolecular chemistry medicine.anatomical_structure chemistry PC-3 Cells Cancer research Molecular Medicine Drug Screening Assays Antitumor |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 30:127454 |
| ISSN: | 0960-894X |
| Popis: | Prostate cancer is an important cause of death in the male population and for which there is no satisfactory chemotherapy. Herein a new series of chalcone hybrids containing 2H-1,2,3-triazole core as the ring B has been synthesized and evaluated in vitro against PC-3 prostate cancer cell line. Compounds 4a, 4c and 4e significantly reduced cell viability and showed IC50 of 28.55, 15.64 and 25.56 µM, respectively. The structure-activity relationship supported by computational chemistry points that the polarity of the molecular surface area should have some relevance to the efficiency of the compounds, in particular the ratio of the partial positive charge sites and the total molecular surface area exposed to the cell environment. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|
Full Text from ScienceDirect