scholarly journals Discovery of (E)-3-((Styrylsulfonyl)methyl)pyridine and (E)-2-((Styrylsulfonyl)methyl)pyridine Derivatives as Anticancer Agents: Synthesis, Structure–Activity Relationships, and Biological Activities

2014 ◽  
Vol 57 (6) ◽  
pp. 2275-2291 ◽  
Author(s):  
Tiangong Lu ◽  
Aik Wye Goh ◽  
Mingfeng Yu ◽  
Julian Adams ◽  
Frankie Lam ◽  
...  
Keyword(s):  
Anticancer Agents ◽  
Biological Activities ◽  
Pyridine Derivatives ◽  
Structure Activity Relationships ◽  
Structure Activity ◽  
Methyl Pyridine

Design, synthesis and biological activities of pyrrole-3-carboxamide derivatives as EZH2 (enhancer of zeste homologue 2) inhibitors and anticancer agents

2020 ◽  
Vol 44 (6) ◽  
pp. 2247-2255
Author(s):  
Qifan Zhou ◽  
Lina Jia ◽  
Fangyu Du ◽  
Xiaoyu Dong ◽  
Wanyu Sun ◽  
...  
Keyword(s):  
Biological Activity ◽  
Anticancer Agents ◽  
Biological Activities ◽  
Activity Assay ◽  
Design Synthesis ◽  
Structure Activity Relationships ◽  
Structure Activity ◽  
Enhancer Of Zeste

A novel series of pyrrole-3-carboxamides targeting EZH2 have been designed and synthesized. The structure–activity relationships were summarized by combining with in vitro biological activity assay and docking results.

Isothiocyanate Synthetic Analogs: Biological Activities, Structure-Activity Relationships and Synthetic Strategies

2014 ◽  
Vol 14 (12) ◽  
pp. 963-977 ◽  
Author(s):  
Andrea Milelli ◽  
Carmela Fimognari ◽  
Nicole Ticchi ◽  
Paolo Neviani ◽  
Anna Minarini ◽  
...  
Keyword(s):  
Biological Activities ◽  
Synthetic Analogs ◽  
Structure Activity Relationships ◽  
Structure Activity

1,3,4-Oxadiazole Containing Compounds As Therapeutic Targets For Cancer Therapy

2021 ◽  
Vol 21 ◽  
Author(s):  
Mohamed Jawed Ahsan
Keyword(s):  
Thermal Stability ◽  
Drug Design ◽  
Anticancer Agents ◽  
Biological Activities ◽  
Molecular Targets ◽  
Docking Simulation ◽  
Premature Death ◽  
Aqueous Solubility ◽  
Molecular Docking Simulation ◽  
Structure Activity

Background: Cancer is the first or second leading cause of premature death in 134 of 183 countries in the world. 1,3,4-Oxadiazoles are five memebered heterocyclic rings containing two nitrogen (two atoms) and oxygen (one atom). They show better thermal stability, metabolic stability, aqueous solubility and lower lipophilicity than the other isomeric oxadiazoles. They are important class of heterocycles present in many drug structures like Raltegravir, Furamizole Tidazosin, Nesapidil, Setileuton (MK-0633) and Zibotentan. Presence of this nucleus in the therapeutics has made them an indispensable anchor for drug design and development. Several 1,3,4-oxadiazoles are prepared and reported as anticancer agents by numerous scientists worldwide. Objectives: The present review discusses the anticancer potentials together with the molecular targets of 1,3,4-oxadiazoles reported since 2010. The structure activity relationship (SAR) and molecular docking simulation on different targets have also been discussed herein. Some of the important cancer targets have also been explored. Methods: The most potent 1,3,4-oxadiazoles reported in literature was highlighted in the manuscript. The anticancer activity was reported in terms of growth percent (GP), percent growth inhibition (%GI), GI50, IC50, and LC50 and TGI. Results: 1,3,4-Oxadiazoles are an important heterocyclic scaffolds with broad spectrum biological activities. They may be either mono substituted or disubstituted and act as an indispensable anchor for drug design and discovery due to their thermal stability together with low lipophilicity. They exhibited anticancer potentials and showed the inhibitions of various cancer targets. Conclusion: The discussion outlined herein will proved to be a helpful and vital tool for medicinal chemists investigating and working with 1,3,4-oxadiazoles and anticancer research programs.

scholarly journals Hybrid cis-stilbene Molecules: Novel Anticancer Agents

2019 ◽  
Vol 20 (6) ◽  
pp. 1300 ◽  
Author(s):  
Natalia Piekuś-Słomka ◽  
Renata Mikstacka ◽  
Joanna Ronowicz ◽  
Stanisław Sobiak
Keyword(s):  
Anticancer Agents ◽  
Biological Activities ◽  
Distinct Group ◽  
Design Synthesis ◽  
Drug Candidates ◽  
Structure Activity ◽  
Polymerization Inhibitor ◽  
Hybrid Molecules ◽  
Tubulin Polymerization Inhibitor ◽  
Pharmacologically Active

The growing interest in anticancer hybrids in the last few years has resulted in a great number of reports on hybrid design, synthesis and bioevaluation. Many novel multi-target-directed drug candidates were synthesized, and their biological activities were evaluated. For the design of anticancer hybrid compounds, the molecules of stilbenes, aromatic quinones, and heterocycles (benzimidazole, imidazole, pyrimidine, pyridine, pyrazole, quinoline, quinazoline) were applied. A distinct group of hybrids comprises the molecules built with natural compounds: Resveratrol, curcumin, coumarin, and oleanolic acid. In this review, we present the studies on bioactive hybrid molecules of a well-known tubulin polymerization inhibitor, combretastatin A-4 and its analogs with other pharmacologically active entities. The mechanism of anticancer activity of selected hybrids is discussed considering the structure-activity relationship.

5-Cinnamoyl-6-aminouracil derivatives as novel anticancer agents. Synthesis, biological evaluation, and structure-activity relationships

1985 ◽  
Vol 28 (4) ◽  
pp. 497-502 ◽  
Author(s):  
Jean Luc Bernier ◽  
Jean Pierre Henichart ◽  
Vincent Warin ◽  
Chantal Trentesaux ◽  
Jean Claude Jardillier
Keyword(s):  
Anticancer Agents ◽  
Biological Evaluation ◽  
Structure Activity Relationships ◽  
Structure Activity
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