RRC ID 73996
Author Ciftci H, Sever B, Kaya N, Bayrak N, Yıldız M, Yıldırım H, Tateishi H, Otsuka M, Fujita M, TuYuN AF.
Title Studies on 1,4-Quinone Derivatives Exhibiting Anti-Leukemic Activity along with Anti-Colorectal and Anti-Breast Cancer Effects.
Journal Molecules
Abstract Colorectal cancer (CRC), breast cancer, and chronic myeloid leukemia (CML) are life-threatening malignancies worldwide. Although potent therapeutic and screening strategies have been developed so far, these cancer types are still major public health problems. Therefore, the exploration of more potent and selective new agents is urgently required for the treatment of these cancers. Quinones represent one of the most important structures in anticancer drug discovery. We have previously identified a series of quinone-based compounds (ABQ-1-17) as anti-CML agents. In the current work, ABQ-3 was taken to the National Cancer Institute (NCI) for screening to determine its in vitro antiproliferative effects against a large panel of human tumor cell lines at five doses. ABQ-3 revealed significant growth inhibition against HCT-116 CRC and MCF-7 breast cancer cells with 2.00 µM and 2.35 µM GI50 values, respectively. The MTT test also showed that ABQ-3 possessed anticancer effects towards HCT-116 and MCF-7 cells with IC50 values of 5.22 ± 2.41 μM and 7.46 ± 2.76 μM, respectively. Further experiments indicated that ABQ-3 induced apoptosis in both cell lines, and molecular docking studies explicitly suggested that ABQ-3 exhibited DNA binding in a similar fashion to previously reported compounds. Based on in silico pharmacokinetic prediction, ABQ-3 might display drug-like features enabling this compound to become a lead molecule for future studies.
Volume 28(1)
Published 2022-12-22
DOI 10.3390/molecules28010077
PII molecules28010077
PMID 36615273
PMC PMC9822417
MeSH Antineoplastic Agents* / chemistry Antineoplastic Agents* / pharmacology Cell Line, Tumor Cell Proliferation Dose-Response Relationship, Drug Drug Screening Assays, Antitumor Humans Molecular Docking Simulation Molecular Structure Neoplasms* Quinones / pharmacology Structure-Activity Relationship
IF 3.267
Resource
Human and Animal Cells HCT116(RCB2979)