Synthesis and SAR studies of phenanthroindolizidine and phenanthroquinolizidine alkaloids as potent anti-tumor agents.

  title={Synthesis and SAR studies of phenanthroindolizidine and phenanthroquinolizidine alkaloids as potent anti-tumor agents.},
  author={Ziwen Wang and Meng Wu and Yi Wang and Zheng Li and Lei Wang and Guifang Han and Fazhong Chen and Yuxiu Liu and Kailiang Wang and Ao Zhang and Linghua Meng and Qingmin Wang},
  journal={European journal of medicinal chemistry},
6-OH-Phenanthroquinolizidine Alkaloid and Its Derivatives Exert Potent Anticancer Activity by Delaying S Phase Progression.
A mechanistic evaluation showed that 2-R potently inhibited cell growth and colony formation, which is associated with a delay in S phase progression through the inhibition of DNA synthesis, which will facilitate the discovery of new Phenanthroindolizidine and phenanthroquinolIZidine alkaloids for use as anticancer drug candidates.
First Discovery and Stucture-Activity Relationship Study of Phenanthroquinolizidines as Novel Antiviral Agents against Tobacco Mosaic Virus (TMV)
Fundamental support for development and optimization of phenanthroquinolizidine alkaloids as potential inhibitors of plant virus is provided.
Different salt derivatives of phenanthroindolizidine alkaloids display different in vitro antitumor activity
Salification is most commonly employed for modifying physical and chemical properties. However, there are few reports on the differences in biological activity between different salt forms and free
Synthesis and Antitumor Activity Evaluation of New Phenanthrene-Based Tylophorine Derivatives
A series of new phenanthrene-based tylophorine derivatives (PBTs) were synthesized in good yield and their structures were characterized by 1H-NMR spectroscopy and ESI MS, and the structure-activity relationship of these compounds was discussed based on the results of their antitumor activity.
Phenanthrotriazine Derivatives Containing Arylidine Hydrazone Moieties as Novel Potential c-Met Inhibitors with Anticancer Effect
Phenanthrene 1,2,4-triazines, especially the ones with less influence on normal cells, may constitute promising compounds for the discovery of antiproliferative agents with potential c-Met inhibitory capacity.
In vitro anticancer effects of two novel phenanthroindolizidine alkaloid compounds on human colon and liver cancer cells
Chemical structure modifications of natural PAs based on anticancer activity assessments may be feasible in the development of new cancer chemotherapeutic agents.
Screening of Phenanthroquinolizidine Alkaloid Derivatives for Inducing Cell Death of L1210 Leukemia Cells with Negative and Positive P-glycoprotein Expression
The screening of a set of cryptopleurine derivatives and (epi-)benzo analogs with bioactive phenanthroquinolizidine alkaloids that induce cytotoxic effects in the mouse lymphocytic leukemia cell line L1210 revealed that the most effective derivative 11 effectively induced cell death in S, R and T cells at similar inhibitory concentrations independent of P-gp expression.


Structure-activity studies of phenanthroindolizidine alkaloids as potential antitumor agents.
Phenanthroindolizidines and Phenanthroquinolizidines: Promising Alkaloids for Anti-Cancer Therapy.
  • S. Chemler
  • Chemistry, Biology
    Current bioactive compounds
  • 2009
This review will highlight important contributions to the isolation, synthesis, SAR and mechanism of action of the phenanthroindolizidine and pheanthroquinolIZidine alkaloids.
Synthesis and structure-activity studies of antofine analogues as potential anticancer agents.
Novel Mode of Action of Tylophorine Analogs as Antitumor Compounds
These tylophorine analogs are a unique class of antitumor compounds that have a mode of action different from known antitumors, and had an inhibitory effect on cyclic AMP response elements, activator protein-1 sites, or nuclear factor-κB binding site-mediated transcriptions.
Antitumor agents 288: design, synthesis, SAR, and biological studies of novel heteroatom-incorporated antofine and cryptopleurine analogues as potent and selective antitumor agents.
Mechanism of action (MOA) studies suggested that R-antofine promotes dysregulation of DNA replication during early S phase, while no similar effects were observed for 11 and 15 on corresponding replication initiation complexes.
Anti-Inflammatory Mechanisms of Phenanthroindolizidine Alkaloids
NSTP0G01 exerts its anti-inflammatory effects by inhibiting expression of the proinflammatory factors and related signaling pathways by blocking mitogen-activated protein/extracellular signal-regulated kinase kinase 1 activity and its downstream signaling activation of NF-κB and AP1.
Phenanthroindolizidine alkaloids from the stems of Ficus septica.
Eight new alkaloids, namely, ficuseptines B-D (1-3), 10R,13aR-tylophorine N-oxide (4, 5, 6, 7, and 8), and 10S, 13aS-isotylocrebrine (8) were isolated from a methanol extract of the stems of Ficus septica by means of spectroscopic data interpretation.
Indolizidine and quinolizidine alkaloids.
  • J. Michael
  • Chemistry, Biology
    Natural product reports
  • 2007
This review covers the isolation, structure determination, synthesis, chemical transformations and biological activity of indolizidine and quinolizidine alkaloids. Included in the review are the