scholarly journals Monocyclic Quinone Structure‐Activity Patterns: Synthesis of Catalytic Inhibitors of Topoisomerase II with Potent Antiproliferative Activity

ChemMedChem ◽  
2019 ◽  
Vol 15 (1) ◽  
pp. 114-124
Author(s):  
Thomas M. Waugh ◽  
John Masters ◽  
Abil E. Aliev ◽  
Charles M. Marson
Keyword(s):  
Antiproliferative Activity ◽  
Topoisomerase Ii ◽  
Activity Patterns ◽  
Structure Activity ◽  
Quinone Structure

scholarly journals Semi-Synthesis of Harringtonolide Derivatives and Their Antiproliferative Activity

Molecules ◽  
2021 ◽  
Vol 26 (5) ◽  
pp. 1380
Author(s):  
Xiutao Wu ◽  
Lijie Gong ◽  
Chen Chen ◽  
Ye Tao ◽  
Wuxi Zhou ◽  
...  
Keyword(s):  
Antiproliferative Activity ◽  
Normal Cell ◽  
Selectivity Index ◽  
Cytotoxic Activities ◽  
Structure Activity ◽  
Growth Inhibitory ◽  
Growth Inhibitory Activity ◽  
Hct 116 ◽  
Systematic Structure

Harringtonolide (HO), a natural product isolated from Cephalotaxus harringtonia, exhibits potent antiproliferative activity. However, little information has been reported on the systematic structure−activity relationship (SAR) of HO derivatives. Modifications on tropone, lactone, and allyl positions of HO (1) were carried out to provide 17 derivatives (2–13, 11a–11f). The in vitro antiproliferative activity against four cancer cell lines (HCT-116, A375, A549, and Huh-7) and one normal cell line (L-02) was tested. Amongst these novel derivatives, compound 6 exhibited comparable cell growth inhibitory activity to HO and displayed better selectivity index (SI = 56.5) between Huh-7 and L-02 cells. The SAR results revealed that the tropone and lactone moieties are essential for the cytotoxic activities, which provided useful suggestions for further structural optimization of HO.

Antimicrobial Screening, in Silico Studies and QSAR of Chalcone-based 1,4-disubstituted 1,2,3-triazole Hybrids

Drug Research ◽  
2020 ◽  
Author(s):  
Pinki Yadav ◽  
Kashmiri Lal ◽  
Ashwani Kumar
Keyword(s):  
Topoisomerase Ii ◽  
Antimicrobial Properties ◽  
Qsar Model ◽  
Quantitative Structure Activity Relationship ◽  
Binding Modes ◽  
E Coli ◽  
Structure Activity ◽  
In Silico Studies ◽  
Microbial Strains

AbstractThe in vitro antimicrobial properties of some chalcones (1a–1c ) and chalcone tethred 1,4-disubstituted 1,2,3-triazoles (2a–2u) towards different microbial strains viz. Staphylococcus aureus, Bacillus subtilis, Escherichia coli, Pseudomonas aeruginosa, Aspergillus niger and Candida albicans are reported. Compounds 2g and 2u exhibited better potency than the standard Fluconazole with MIC values of 0.0063 µmol/mL and 0.0068 µmol/mL, respectively. Furthermore, molecular docking was performed to investigate the binding modes of two potent compounds 2q and 2g with E. coli topoisomerase II DNA gyrase B and C. albicans lanosterol 14α-demethylase, respectively. Based on these results, a statistically significant quantitative structure activity relationship (QSAR) model was successfully summarized for antibacterial activity against B. subtilis.

scholarly journals Development of CDK4/6 Inhibitors: A Five Years Update

Molecules ◽  
2021 ◽  
Vol 26 (5) ◽  
pp. 1488
Author(s):  
Alessandra Ammazzalorso ◽  
Mariangela Agamennone ◽  
Barbara De Filippis ◽  
Marialuigia Fantacuzzi
Keyword(s):  
Breast Cancer ◽  
Metastatic Breast Cancer ◽  
Adverse Effects ◽  
Antiproliferative Activity ◽  
Treatment Efficacy ◽  
Metastatic Breast ◽  
Breast Cancer Treatment ◽  
Survival Outcomes ◽  
Cyclin Dependent Kinases ◽  
Structure Activity

The inhibition of cyclin dependent kinases 4 and 6 plays a role in aromatase inhibitor resistant metastatic breast cancer. Three dual CDK4/6 inhibitors have been approved for the breast cancer treatment that, in combination with the endocrine therapy, dramatically improved the survival outcomes both in first and later line settings. The developments of the last five years in the search for new selective CDK4/6 inhibitors with increased selectivity, treatment efficacy, and reduced adverse effects are reviewed, considering the small-molecule inhibitors and proteolysis-targeting chimeras (PROTACs) approaches, mainly pointing at structure-activity relationships, selectivity against different kinases and antiproliferative activity.

Antiproliferative activity of cardenolides on cell line A549: structure–activity relationship analysis

2020 ◽  
Author(s):  
Salvador Enrique Meneses-Sagrero ◽  
Luisa Alondra Rascón-Valenzuela ◽  
Rogerio Sotelo-Mundo ◽  
Wagner Vilegas ◽  
Carlos Velazquez ◽  
...  
Keyword(s):  
Cell Line ◽  
Antiproliferative Activity ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Relationship Analysis ◽  
Structure Activity

Imidazopyridine-fused [1,3]-diazepinones part 2: Structure-activity relationships and antiproliferative activity against melanoma cells

2017 ◽  
Vol 125 ◽  
pp. 1225-1234 ◽  
Author(s):  
Virginie Bellet ◽  
Laure Lichon ◽  
Dominique P. Arama ◽  
Audrey Gallud ◽  
Vincent Lisowski ◽  
...  
Keyword(s):  
Antiproliferative Activity ◽  
Melanoma Cells ◽  
Structure Activity Relationships ◽  
Structure Activity

In vitro developmental toxicity of five direct-acting alkylating agents in rodent embryos: Structure-activity patterns

Teratology ◽  
1989 ◽  
Vol 40 (3) ◽  
pp. 199-210 ◽  
Author(s):  
Elaine M. Faustman ◽  
Zamyat Kirby ◽  
Daniel Gage ◽  
Michael Varnum
Keyword(s):  
Developmental Toxicity ◽  
Alkylating Agents ◽  
Activity Patterns ◽  
Structure Activity ◽  
Direct Acting

Structure–Activity Studies on the Spiroketal Moiety of a Simplified Analogue of Debromoaplysiatoxin with Antiproliferative Activity

2012 ◽  
Vol 55 (11) ◽  
pp. 5614-5626 ◽  
Author(s):  
Masayuki Kikumori ◽  
Ryo C. Yanagita ◽  
Harukuni Tokuda ◽  
Nobutaka Suzuki ◽  
Hiroshi Nagai ◽  
...  
Keyword(s):  
Antiproliferative Activity ◽  
Structure Activity
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