ChemInform Abstract: Synthesis of New Chiral 2,5-Disubstituted 1,3,4-Thiadiazoles Possessing γ-Butenolide Moiety and Preliminary Evaluation of in vitro Anticancer Activity.

ChemInform ◽  
2009 ◽  
Vol 40 (39) ◽  
Author(s):  
Meng-Xue Wei ◽  
Lei Feng ◽  
Xue-Qiang Li ◽  
Xue-Zhang Zhou ◽  
Zhi-Hui Shao
Keyword(s):  
Anticancer Activity ◽  
Preliminary Evaluation

Synthesis of Pt(II) complexes of the type [Pt(1,10-phenanthroline)(SArFn)2] (SArFn = SC6H3-3,4-F2; SC6F4-4-H; SC6F5). Preliminary evaluation of their in vitro anticancer activity

2020 ◽  
Vol 211 ◽  
pp. 111206
Author(s):  
Geraldine Backman-Blanco ◽  
Hugo Valdés ◽  
María Teresa Ramírez-Apan ◽  
Patricia Cano-Sanchez ◽  
Simón Hernandez-Ortega ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Preliminary Evaluation

NHC-Ir(I) complexes derived from 5,6-dinitrobenzimidazole. Synthesis, characterization and preliminary evaluation of their in vitro anticancer activity

2019 ◽  
Vol 496 ◽  
pp. 119061 ◽  
Author(s):  
Arturo Sánchez-Mora ◽  
Hugo Valdés ◽  
María Teresa Ramírez-Apan ◽  
Antonio Nieto-Camacho ◽  
Simón Hernández-Ortega ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Preliminary Evaluation

scholarly journals Synthesis and preliminary evaluation of the anti-cancer activity on A549 lung cancer cells of a series of unsaturated disulfides

MedChemComm ◽  
2019 ◽  
Vol 10 (1) ◽  
pp. 116-119 ◽  
Author(s):  
Fabrizio Olivito ◽  
Nicola Amodio ◽  
Maria Luisa Di Gioia ◽  
Monica Nardi ◽  
Manuela Oliverio ◽  
...  
Keyword(s):  
Lung Cancer ◽  
Anticancer Activity ◽  
Cancer Cells ◽  
Lung Cancer Cells ◽  
Preliminary Evaluation ◽  
Natural Analogue ◽  
Anti Cancer ◽  
A549 Lung ◽  
Cancer Activity

In this work we synthesized and tested a series of unsaturated disulfides. Two compounds showed a promising anticancer activity in vitro on A549 lung cancer cells compared to the natural analogue.

Synthesis of Novel Matrine Derivatives Containing Furanone Skeleton and Preliminary Evaluation of Their Anticancer Activity in Vitro

2018 ◽  
Vol 38 (10) ◽  
pp. 2633
Author(s):  
Fuli Ma ◽  
Jiao Zhang ◽  
Ming Li ◽  
Jiaying Yu ◽  
Wei Luo ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Preliminary Evaluation

Synthesis of theophylline-based iridium(I) N-heterocyclic carbene complexes including fluorinated-thiophenolate ligands. Preliminary evaluation of their in vitro anticancer activity

2020 ◽  
Vol 507 ◽  
pp. 119588 ◽  
Author(s):  
Itzel Eslava-Gonzalez ◽  
Hugo Valdés ◽  
María Teresa Ramírez-Apan ◽  
Simón Hernandez-Ortega ◽  
Miriam Rosario Zermeño-Ortega ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Preliminary Evaluation ◽  
Carbene Complexes

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.

Recent Design and Structure-Activity Relationship Studies on Modifications of DHFR Inhibitors as Anticancer Agents

2019 ◽  
Vol 26 ◽  
Author(s):  
Agnieszka Wróbel ◽  
Danuta Drozdowska
Keyword(s):  
Anticancer Activity ◽  
Anticancer Drugs ◽  
Anticancer Agents ◽  
Physicochemical Characterization ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Biological Research ◽  
Structure Activity ◽  
Dhfr Inhibitors

Background: Dihydrofolate reductase (DHFR) has been known for decades as a molecular target for antibacterial, antifungal and anti-malarial treatments. This enzyme is becoming increasingly important in the design of new anticancer drugs, which is confirmed by numerous studies including modelling, synthesis and in vitro biological research. This review aims to present and discuss some remarkable recent advances on the research of new DHFR inhibitors with potential anticancer activity. Methods: The scientific literature of the last decade on the different types of DHFR inhibitors has been searched. The studies on design, synthesis and investigation structure-activity relationship were summarized and divided into several subsections depending on the leading molecule and its structural modification. Various methods of synthesis, potential anticancer activity and possible practical applications as DHFR inhibitors of new chemical compounds were described and discussed. <p> Results: This review presents the current state of knowledge on the modification of known DHFR inhibitors and the structures and searching for over eighty new molecules, designed as potential anticancer drugs. In addition, DHFR inhibitors acting on thymidylate synthase (TS), carbon anhydrase (CA) and even DNA-binding are presented in this paper. <p> Conclusion: Thorough physicochemical characterization and biological investigations it is possible to understand structure-activity relationship of DHFR inhibitors. This will enable even better design and synthesis of active compounds, which would have the expected mechanism of action and the desired activity.

Extraction, Chemical Composition, Antioxidant Property and In vitro Anticancer Activity of Silymarin from Silybum Marianum On Kb and A549 Cell Lines

2020 ◽  
Vol 17 ◽  
Author(s):  
Mojgan Azadpour ◽  
Mohammad Mehdi Farajollahi ◽  
Ali Mohammad Varzi ◽  
Pejman Hashemzadeh ◽  
Hossein Mahmoudvand ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Cell Lines ◽  
A549 Cell ◽  
Hplc Analysis ◽  
Antioxidant Properties ◽  
Radical Scavenging ◽  
Antioxidant Property ◽  
Silybum Marianum ◽  
Stable Free Radical

Introduction: This study aimed to evaluate the antioxidant property of silymarin (SM) extracted from the seed of Silybum marianum and its anticancer activity on KB and A549 cell lines following 24, 48, and 72 h of treatment. Methods: Ten grams of powdered S. marianum seeds were defatted using n-hexane for 6 hours and then extracted by methanol. The silymarin extracted of extraction components The extracted components of silymarin were measured by spectrophotometric assay and HPLC analysis. 2, 2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging, phenol content, total flavonoid content, and total antioxidant capacity were measured to detect the antioxidant properties of SM. The anticancer activity of the SM on cell lines evaluated by MTT. Results: In HPLC analysis, more than 50% of the peaks were related to silibin A and B. SM was reducedDPPH (the stable free radical) with a 50% inhibitory concentration (IC50) of 6.56 μg/ ml in comparison with butylated hydroxyl toluene (BHT), which indicated an IC50 of ~3.9 μg/ ml.The cytotoxicity effect of SM on the cell lines was studied by MTT assay. The cytotoxicity effect of the extracted silymarin on KB and A549 cell lines was observed up to 80 and 70% at 156 and 78 µg/ml, respectively. The IC50 value of the extracted SM on KB and A549 cell lines after 24 hours of treatment was seen at 555 and 511 µg/ml, respectively. Conclusion: Due to the good antioxidant and anticancer properties of the isolated silymarin, its use as an anticancer drug is suggested.

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