ChemInform Abstract: Synthesis, Structure Activity Relationship and Mode of Action of 3-Substitutedphenyl-1- (2,2,8,8-tetramethyl-3,4,9,10-tetrahydro-2H,8H-pyrano [2,3-f]chromen-6-yl)-propenones as Novel Anticancer Agents in Human Leukaemia HL-60 Cells.

ChemInform ◽  
2013 ◽  
Vol 44 (33) ◽  
pp. no-no
Author(s):  
Y. L. N. Murthy ◽  
K. P. Suhasini ◽  
A. S. Pathania ◽  
S. Bhushan ◽  
Y. Nagendra Sastry
Keyword(s):  
Anticancer Agents ◽  
Mode Of Action ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Structure Activity ◽  
Human Leukaemia

A mode of action study of cationic anthraquinone analogs: a new class of highly potent anticancer agents

MedChemComm ◽  
2015 ◽  
Vol 6 (11) ◽  
pp. 2012-2022 ◽  
Author(s):  
Jaya P. Shrestha ◽  
Yagya Prasad Subedi ◽  
Liaohai Chen ◽  
Cheng-Wei Tom Chang
Keyword(s):  
Cancer Cells ◽  
Anticancer Agents ◽  
Mode Of Action ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
New Class ◽  
Structure Activity ◽  
Sar Study

Previously, we reported the synthesis and structure–activity relationship (SAR) study of a series of novel 4,9-dioxo-4,9-dihydro-1H-naphtho[2,3-d][1,2,3]triazol-3-ium salts, which had very potent anti-proliferative activities (low μM to nM GI50) against a broad range of cancer cells.

Biological Activity of Trans-Membrane Anion Carriers

2018 ◽  
Vol 25 (30) ◽  
pp. 3560-3576 ◽  
Author(s):  
Massimo Tosolini ◽  
Paolo Pengo ◽  
Paolo Tecilla
Keyword(s):  
Biological Activity ◽  
Membrane Transport ◽  
Anticancer Agents ◽  
Biological Effects ◽  
Structure Activity Relationship ◽  
New Drugs ◽  
Activity Relationship ◽  
Anion Channels ◽  
Cellular Homeostasis ◽  
Structure Activity

Natural and synthetic anionophores promote the trans-membrane transport of anions such as chloride and bicarbonate. This process may alter cellular homeostasis with possible effects on internal ions concentration and pH levels triggering several and diverse biological effects. In this article, an overview of the recent results on the study of aniontransporters, mainly acting with a carrier-type mechanism, is given with emphasis on the structure/activity relationship and on their biological activity as antibiotic and anticancer agents and in the development of new drugs for treating conditions derived from dysregulation of natural anion channels.

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.

Triazol: a privileged scaffold for proteolysis targeting chimeras

2019 ◽  
Vol 11 (22) ◽  
pp. 2919-2973 ◽  
Author(s):  
Li-Wen Xia ◽  
Meng-Yu Ba ◽  
Wei Liu ◽  
Weyland Cheng ◽  
Chao-Ping Hu ◽  
...  
Keyword(s):  
Drug Discovery ◽  
Anticancer Activity ◽  
Mode Of Action ◽  
Critical Analysis ◽  
Enzyme Inhibitors ◽  
Structure Activity Relationship ◽  
Target Protein ◽  
Activity Relationship ◽  
Structure Activity ◽  
Privileged Scaffold

Current traditional drugs such as enzyme inhibitors and receptor agonists/antagonists present inherent limitations due to occupancy-driven pharmacology as the mode of action. Proteolysis targeting chimeras (PROTACs) are composed of an E3 ligand, a connecting linker and a target protein ligand, and are an attractive approach to specifically knockdown-targeted proteins utilizing an event-driven mode of action. The length, hydrophilicity and rigidity of connecting linkers play important role in creating a successful PROTAC. Some PROTACs with a triazole linker have displayed promising anticancer activity. This review provides an overview of PROTACs with a triazole scaffold and discusses its structure–activity relationship. Important milestones in the development of PROTACs are addressed and a critical analysis of this drug discovery strategy is also presented.

Structure-Activity Relationship Analyses of Glycyrrhetinic Acid Derivatives as Anticancer Agents

2011 ◽  
Vol 11 (10) ◽  
pp. 881-887 ◽  
Author(s):  
B. Lallemand ◽  
M. Gelbcke ◽  
J. Dubois ◽  
M. Prevost ◽  
I. Jabin ◽  
...  
Keyword(s):  
Anticancer Agents ◽  
Structure Activity Relationship ◽  
Glycyrrhetinic Acid ◽  
Activity Relationship ◽  
Structure Activity

scholarly journals Antitubercular 2-Pyrazolylpyrimidinones: Structure–Activity Relationship and Mode-of-Action Studies

2021 ◽  
Author(s):  
Candice Soares de Melo ◽  
Vinayak Singh ◽  
Alissa Myrick ◽  
Sandile B. Simelane ◽  
Dale Taylor ◽  
...  
Keyword(s):  
Mode Of Action ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Structure Activity
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