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Design and synthesis of various quinizarin derivatives as potential anticancer agents in acute T lymphoblastic leukemia.

Abstract
A series of quinizarin derivatives containing quaternary ammonium salts and/or thiourea groups were synthesized and their anticancer activities against leukemia cell lines have been tested. Results showed that most of quinizarin derivatives could inhibit the proliferation of leukemia cells. Among these derivatives, compound 3 showed good inhibition activity against various leukemia cells with IC50 values ranging from 0.90 ± 2.55 μM to 10.90 ± 3.66 μM. At the same time, compound 3 also inhibited the growth of human embryonic kidney-293 cell (HEK-293). Molt-4 and Jurkat cells, acute T lymphoblastic leukemia (T-ALL) cell lines, were selected to reveal potential anticancer mechanism of compound 3. Compound 3 inhibited the proliferation of Molt-4 and Jurkat cells in a dose- and time-dependent manner and led to a marked G0/G1 phase arrest. Analysis of Annexin V-APC and intracellular reactive oxygen species (ROS) level by flow cytometry showed that compound 3 induced significant apoptosis in Molt-4 and Jurkat cells. Western blotting assay showed that compound 3 activated the caspase-dependent apoptosis pathway and induced the degradation of Bcl-2 and c-myc protein.
AuthorsXiufang Hu, Yanqin Cao, Xu Yin, Li Zhu, Yingyu Chen, Wenfeng Wang, Jianda Hu
JournalBioorganic & medicinal chemistry (Bioorg Med Chem) Vol. 27 Issue 7 Pg. 1362-1369 (04 01 2019) ISSN: 1464-3391 [Electronic] England
PMID30827866 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
CopyrightCopyright © 2019 Elsevier Ltd. All rights reserved.
Chemical References
  • Anthraquinones
  • Antineoplastic Agents
  • 1,4-dihydroxyanthraquinone
Topics
  • Anthraquinones (chemical synthesis, chemistry, pharmacology)
  • Antineoplastic Agents (chemical synthesis, chemistry, pharmacology)
  • Cell Cycle (drug effects)
  • Cell Line, Tumor
  • Cell Proliferation (drug effects)
  • Dose-Response Relationship, Drug
  • Drug Design
  • Humans
  • Jurkat Cells
  • Molecular Structure
  • Precursor Cell Lymphoblastic Leukemia-Lymphoma (drug therapy, metabolism, pathology)
  • Structure-Activity Relationship

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