Marine pyridoacridine alkaloids and synthetic analogues as antitumor agents

2002 ◽  
Vol 23 (2) ◽  
pp. 234-252 ◽  
Author(s):  
Evelyne Delfourne ◽  
Jean Bastide
Keyword(s):  
Antitumor Agents ◽  
Synthetic Analogues ◽  
Pyridoacridine Alkaloids

Semi-synthesis as a tool for broadening the health applications of bioactive olive secoiridoids: a critical review

2021 ◽  
Author(s):  
Manuela Oliverio ◽  
Monica Nardi ◽  
Maria Luisa Di Gioia ◽  
Paola Costanzo ◽  
Sonia Bonacci ◽  
...  
Keyword(s):  
Critical Review ◽  
Natural Compounds ◽  
Effective Strategy ◽  
Synthetic Analogues ◽  
Health Applications ◽  
Natural And Synthetic

Semi-synthesis is an effective strategy to obtain both natural and synthetic analogues of the olive secoiridoids, starting from easy accessible natural compounds.

SUBACUTE THYROIDITIS

1960 ◽  
Vol XXXIII (III) ◽  
pp. 457-472 ◽  
Author(s):  
B.-A. Lamberg ◽  
G. Hintze ◽  
R. Jussila ◽  
M. Berlin
Keyword(s):  
Thyroid Function ◽  
Early Phase ◽  
Radioactive Iodine ◽  
Serum Proteins ◽  
Conversion Ratio ◽  
Subacute Thyroiditis ◽  
Synthetic Analogues ◽  
The Third ◽  
Thyroid Uptake ◽  
Iodine Metabolism

ABSTRACT A series of cases of clinically diagnosed subacute thyroiditis comprising 11 patients is reported. Studies on the iodine metabolism, electrophoretic distribution of the serum proteins and the responsiveness to TSH were carried out. The patients were observed for periods up to 16 months from the onset of the disease. In the early phase there was an elevation of the serum PBI in a few cases and hyperthyroid signs in some, accompanied by depressed thyroid uptake of radioactive iodine and a fairly good response to TSH. Later, the thyroid grew hard and the iodine metabolism changed. In several cases there was a marked increase in the conversion ratio and the serum PB131I level. The responses to TSH was variable for different parameters of thyroid function, suggesting a state of »low thyroid reserve« as defined by Jefferies et al. (1956). Hypothyroidism developed in 3 cases; in two of them there was a response to exogenous TSH, in the third no response was seen at this stage of the disease. Cortisone and synthetic analogues seem to be of great benefit in the treatment of the acute symptoms of the disease.

Vitamin D as potential therapeutic anticancer agent

2018 ◽  
pp. 1-3
Keyword(s):  
Vitamin D ◽  
Anticancer Activity ◽  
Anticancer Agent ◽  
Antitumor Agents ◽  
Metastatic Potential ◽  
Anticancer Properties ◽  
Chemotherapy Agents

The role of vitamin D is implicated in carcinogenesis through numerous biological processes like induction of apoptosis, modulation of immune system inhibition of inflammation and cell proliferation and promotion of cell differentiation. Its use as additional adjuvant drug with cancer treatment may be novel combination for improved outcome of different cancers. Numerous preclinical, epidemiological and clinical studies support the role of vitamin D as an anticancer agent. Anticancer properties of vitamin D have been studied widely (both in vivo and in vitro) among various cancers and found to have promising results. There are considerable data that indicate synergistic potential of calcitriol and antitumor agents. Possible mechanisms for modulatory anticancer activity of vitamin D include its antiproliferative, prodifferentiating, and anti-angiogenic and apoptic properties. Calcitriol reduces invasiveness and metastatic potential of many cancer cells by inhibiting angiogenesis and regulating expression of the key molecules involved in invasion and metastasis. Anticancer activity of vitamin D is synergistic or additive with the antineoplastic actions of several drugs including cytotoxic chemotherapy agents like paclitaxel, docetaxel, platinum base compounds and mitoxantrone. Benefits of addition of vitamin D should be weighed against the risk of its toxicity.

Oxazole: A Promising Building Block for the Development of Potent Antitumor Agents

2016 ◽  
Vol 16 (30) ◽  
pp. 3582-3589 ◽  
Author(s):  
Hua Zhou ◽  
Jiang-Qun Cheng ◽  
Zhi-Sen Wang ◽  
Fei-Hu Chen ◽  
Xin-Hua Liu
Keyword(s):  
Building Block ◽  
Antitumor Agents

Design, Synthesis, In vitro and In silico Evaluation of New Hydrazonebased Antitumor Agents as Potent Akt Inhibitors

2020 ◽  
Vol 17 (11) ◽  
pp. 1380-1392
Author(s):  
Emine Merve Güngör ◽  
Mehlika Dilek Altıntop ◽  
Belgin Sever ◽  
Gülşen Akalın Çiftçi
Keyword(s):  
Cell Line ◽  
Anticancer Agents ◽  
In Silico ◽  
Antitumor Agents ◽  
Colorimetric Assay ◽  
Fibroblast Cell ◽  
Lipinski’S Rule ◽  
In Silico Docking ◽  
Embryonic Fibroblast

Background: Akt is overexpressed or activated in a variety of human cancers, including gliomas, lung, breast, ovarian, gastric and pancreatic carcinomas. Akt inhibition leads to the induction of apoptosis and inhibition of tumor growth and therefore extensive efforts have been devoted to the discovery of potent antitumor drugs targeting Akt. Objectives: The objective of this work was to identify potent anticancer agents targeting Akt. Methods: New hydrazone derivatives were synthesized and investigated for their cytotoxic effects on 5RP7 H-ras oncogene transformed rat embryonic fibroblast and L929 mouse embryonic fibroblast cell lines. Besides, the apoptotic effects of the most active compounds on 5RP7 cell line were evaluated using flow cytometry. Their Akt inhibitory effects were also investigated using a colorimetric assay. In silico docking and Absorption, Distribution, Metabolism and Excretion (ADME) studies were also performed using Schrödinger’s Maestro molecular modeling package. Results and Discussion: Compounds 3a, 3d, 3g and 3j were found to be effective on 5RP7 cells (with IC50 values of <0.97, <0.97, 1.13±0.06 and <0.97 μg/mL, respectively) when compared with cisplatin (IC50= 1.87±0.15 μg/mL). It was determined that these four compounds significantly induced apoptosis in 5RP7 cell line. Among them, N'-benzylidene-2-[(4-(4-methoxyphenyl)pyrimidin- 2-yl)thio]acetohydrazide (3g) significantly inhibited Akt (IC50= 0.5±0.08 μg/mL) when compared with GSK690693 (IC50= 0.6±0.05 μg/mL). Docking studies suggested that compound 3g showed good affinity to the active site of Akt (PDB code: 2JDO). According to in silico ADME studies, the compound also complies with Lipinski's rule of five and Jorgensen's rule of three. Conclusion: Compound 3g stands out as a potential orally bioavailable cytotoxic agent and apoptosis inducer targeting Akt.

Design, Synthesis of Novel Quinazolone Alkaloids Derivatives as Potential Antitumor Agents

2011 ◽  
Vol 7 (4) ◽  
pp. 295-300
Author(s):  
Youguang Zheng ◽  
Min Sun ◽  
Yi Liu ◽  
Mingdong Li ◽  
Min Ji
Keyword(s):  
Antitumor Agents ◽  
Design Synthesis ◽  
Potential Antitumor
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