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

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.

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

Current Medicinal Chemistry ◽

10.2174/0929867326666191016151018 ◽

2019 ◽

Vol 26 ◽

Cited By ~ 1

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.

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Synthesis, structure–activity relationship of novel substituted 4H-chromen-1,2,3,4-tetrahydropyrimidine-5-carboxylates as potential anti-mycobacterial and anticancer agents

Bioorganic & Medicinal Chemistry Letters ◽

10.1016/j.bmcl.2011.03.079 ◽

2011 ◽

Vol 21 (10) ◽

pp. 2855-2859 ◽

Cited By ~ 70

Author(s):

B. China Raju ◽

R. Nageswara Rao ◽

P. Suman ◽

P. Yogeeswari ◽

D. Sriram ◽

...

Keyword(s):

Anticancer Agents ◽

Structure Activity Relationship ◽

Activity Relationship ◽

Structure Activity ◽

Relationship Of

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ChemInform Abstract: Synthesis, Quantitative Structure-Activity Relationship and Biological Evaluation of 1,3,4-Oxadiazole Derivatives Possessing Diphenylamine Moiety as Potential Anticancer Agents.

ChemInform ◽

10.1002/chin.201329144 ◽

2013 ◽

Vol 44 (29) ◽

pp. no-no

Author(s):

Doaa Ezzat Abdel Rahman

Keyword(s):

Anticancer Agents ◽

Quantitative Structure Activity Relationship ◽

Structure Activity Relationship ◽

Biological Evaluation ◽

Activity Relationship ◽

Quantitative Structure ◽

Structure Activity ◽

Oxadiazole Derivatives

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Anticancer agents based on Plastoquinone analogs with N-phenylpiperazine: Structure-activity relationship and mechanism of action in breast cancer cells

Chemico-Biological Interactions ◽

10.1016/j.cbi.2021.109673 ◽

2021 ◽

pp. 109673

Author(s):

Ayse Tarbin Jannuzzi ◽

Mahmut Yıldız ◽

Nilüfer Bayrak ◽

Hatice Yıldırım ◽

Deepak Shilkar ◽

...

Keyword(s):

Breast Cancer ◽

Cancer Cells ◽

Mechanism Of Action ◽

Anticancer Agents ◽

Breast Cancer Cells ◽

Structure Activity Relationship ◽

Activity Relationship ◽

Structure Activity

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Current status of novel pyridine fused derivatives as anticancer agents: An insight into future perspectives and structure activity relationship (SAR)

Current Topics in Medicinal Chemistry ◽

10.2174/1568026621666210916171015 ◽

2021 ◽

Vol 21 ◽

Author(s):

Ajay Manaithiya ◽

Ozair Alam ◽

Vrinda Sharma ◽

Mohd. Javed Naim ◽

Shruti Mittal ◽

...

Keyword(s):

Anticancer Activity ◽

Anticancer Agents ◽

Heterocyclic Ring ◽

Structure Activity Relationship ◽

Activity Relationship ◽

Current Status ◽

Normal Tissues ◽

Structure Activity ◽

Prevalent Disease

: Cancer is a heterogeneous disease characterized by an abnormal and uncontrolled division of the cells leading to tumors that invade the adjacent normal tissues. After cardiovascular diseases, it is the second most prevalent disease accounting for one in every six deaths worldwide. This alarming rate thus, demands an urgent need to investigate more effective drugs to combat the said disease. Oxygen and nitrogen-based heterocyclic compounds have shown remarkable therapeutic activity towards several diseases, including cancer. In this review, we have attempted to summarize the work done in the last decade (2009-2019), highlighting the anticancer activity of pyrido fused five-membered heterocyclic ring derivatives. Additionally, we have focused on seven heterocyclic pyridine fused rings: Imidazopyridine, Triazolopyridine, Pyrrolopyridine, Pyrazolopyridines, Thienopyridine, and Isoxazolopyridine. A total of forty-nine compounds have been studied based on their in-vitro cytotoxic activity and their structure-activity relationship, underlining the anticancer activity of their various pharmacophores and substituents. This review, therefore, aims to draw the attention of the researchers worldwide towards the enormous scope of development of heterocyclic drug compounds, focussing mainly on pyrido fused five-membered heterocyclic rings as anticancer drugs.

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