Bis-triazole-containing compounds with anticancer potential: A short review

2021 ◽  
Vol 21 ◽  
Author(s):  
Meixiang Gao ◽  
Qiang Diao ◽  
Feng Gao ◽  
Xiangyang Sun ◽  
Jiaqi Xiao
Keyword(s):  
Drug Resistance ◽  
Anticancer Agents ◽  
High Efficiency ◽  
Short Review ◽  
Tumor Proliferation ◽  
Invasion And Metastasis ◽  
Drug Candidates ◽  
Structure Activity ◽  
Set Up ◽  
Biological Spectrum

: The development of novel anticancer agents with high efficiency is of great importance due to the severe anticancer scenario of the currently used drugs. Dimerization is a useful method to develop new drug candidates with a broad biological spectrum, enhanced activity and potency to overcome drug resistance. A wide variety of bis-triazole-containing compounds have been developed with improved properties compared with their parent compounds. These derivatives could inhibit tumor proliferation, invasion and metastasis, revealing their potential as putative anticancer candidates. This review covers the recent advances of bis-triazole-containing compounds as anticancer candidates, and the structure-activity relationship are also discussed to set up the direction for the design and development of bis-triazole-containing compounds with higher efficiency.

Quinoline-based compounds with potential activity against drug-resistant cancers

2020 ◽  
Vol 20 ◽  
Author(s):  
Huan-Ting Li ◽  
Xiaoyong Zhu
Keyword(s):  
Drug Resistance ◽  
Anticancer Agents ◽  
Anticancer Agent ◽  
Short Review ◽  
Therapeutic Strategies ◽  
Mechanisms Of Action ◽  
Review Article ◽  
Drug Resistant ◽  
Structure Activity ◽  
Potential Activity

: Drug resistance is the major cause of the failure of cancer chemotherapy, so one of the most important features in developing effective cancer therapeutic strategies is to overcome drug resistance. Quinoline moiety has become one of the most privileged structural motifs in anticancer agent discovery since its derivatives possess potential activity against various cancers including drug-resistant cancers. Several quinoline-based compounds which are represented by Anlotinib, Bosutinib, Lenvatinib, and Neratinib have already been applied in clinical practice to fight against cancers, so quinoline-based compounds are potential anticancer agents. The present short review article provides an overview about the recent advances of quinoline-based compounds with potential activity against drug-resistant cancers. The structure-activity relationship and mechanisms of action are also discussed.

Recent Development of Sulfonyl or Sulfonamide Hybrids as Potential Anticancer Agents: A Key Review

2018 ◽  
Vol 18 (4) ◽  
pp. 488-505 ◽  
Author(s):  
K. P. Rakesh ◽  
Shi-Meng Wang ◽  
Jing Leng ◽  
L. Ravindar ◽  
Abdullah M. Asiri ◽  
...  
Keyword(s):  
Drug Resistance ◽  
Anticancer Agents ◽  
Side Effect ◽  
Docking Studies ◽  
Multi Drug Resistance ◽  
Anticancer Activities ◽  
Pharmacological Activities ◽  
Synthetic Compounds ◽  
Structure Activity ◽  
Anticancer Drug Discovery

Cancer is the second leading cause of death worldwide. There is always a huge demand for novel anticancer drugs and diverse new natural or synthetic compounds are developed continuously by scientists. Presently, a large number of drugs in clinical practice have showed pervasive side effect and multidrug resistance. Sulfonyl or sulfonamide hybrids became one of the most attractive subjects due to their broad spectrum of pharmacological activities. Sulfonyl hybrids were broadly explored for their anticancer activities and it was found that they possess minimum side effect along with multi-drug resistance activity. This review describes the most recent applications of sulfonyl hybrid analogues in anticancer drug discovery and further discusses the mechanistic insights, structure-activity relationships and molecular docking studies for the potent derivatives.

scholarly journals Knigth's Move in the Periodic Table, From Copper to Platinum, Novel Antitumor Mixed Chelate Copper Compounds, Casiopeinas, Evaluated by an in Vitro Human and Murine Cancer Cell Line Panel

2001 ◽  
Vol 8 (1) ◽  
pp. 19-28 ◽  
Author(s):  
Isabel Gracia-Mora ◽  
Lena Ruiz-Ramírez ◽  
Celedonio Gómez-Ruiz ◽  
Mabel Tinoco-Méndez ◽  
Adriana Márquez-Quiñones ◽  
...  
Keyword(s):  
Cancer Cell ◽  
Anticancer Agents ◽  
Human Cancer ◽  
Cancer Cell Line ◽  
Drug Candidates ◽  
Control Drug ◽  
Copper Compounds ◽  
Structure Activity ◽  
Cell Line Panel

We synthesized a novel anticancer agents based on mixed chelate copper (II) complexes, named Casiopeínas® has of general formula [Cu(N-N)(N-O)H2O]NO3 (where, N-N = diimines as 1,10- phenanthroline, 2,2-bipyridine, or substituted and N-O=aminoeidate or [Cu(N-N)(O-O)H2O]NO3 (where NN= diimines as 10-phenanthroline, 2,2-bipyridine or substituted Casiopeínas I, II, IV, V, VI, VII VIII and O-O=acetylacetonate, salicylaldehidate Casiopínas III). We evaluated the in vitro antitumor activity using a human cancer cell panel and some nurine cancer cells. Eleven Casiopeinas are evaluated in order to acquire some structure-activity correlations and some monodentated Casiopeinäs analogues; cisplatinum was used as control drug. The 50% growth inhibition observed is, in all cases reach with concentrations of Casiopeina's 10 or 100 times lower than cisplatinum. In a previous work we reported the induction of apoptosis by Casiopeina II. The results indicate that Casiopeinass are a promising new anticancer drug candidates to be developed further toward clinical trials.

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.

Triazole-containing hybrids with anti-Mycobacterium tuberculosis potential – Part I: 1,2,3-Triazole

2021 ◽  
Author(s):  
Zhenyou Tan ◽  
Jun Deng ◽  
Qiongxian Ye ◽  
Zhenfeng Zhang
Keyword(s):  
Drug Resistance ◽  
Mycobacterium Tuberculosis ◽  
Rational Design ◽  
Multidrug Therapy ◽  
Resistance Development ◽  
Drug Candidates ◽  
Structure Activity ◽  
Privileged Structure ◽  
Potential Part ◽  
Potential Activity

Tuberculosis regimens currently applied in clinical practice require months of multidrug therapy, which imposes a major challenge of patient compliance and drug resistance development. Moreover, because of the increasing emergence of hard-to-treat tuberculosis, this disease continues to be a significant threat to the human population. 1,2,3-triazole as a privileged structure has been widely used as an effective template for drug discovery, and 1,2,3-triazole-containing hybrids that can simultaneously act on dual or multiple targets in Mycobacterium tuberculosis have the potential to circumvent drug resistance, enhance efficacy, reduce side effects and improve pharmacokinetic as well as pharmacodynamic profiles. Thus, 1,2,3-triazole-containing hybrids are useful scaffolds for the development of antitubercular agents. This review aims to highlight recent advances of 1,2,3-triazole-containing hybrids with potential activity against various forms of M. tuberculosis, covering articles published between 2015 and 2020. The structure–activity relationship and the mechanism of action are also discussed to facilitate further rational design of more effective drug candidates.

β-Lactone derivatives and their anticancer activities: A short review

2021 ◽  
Vol 21 ◽  
Author(s):  
Jun Wang ◽  
Yumin Shi ◽  
Dan Jiang
Keyword(s):  
Drug Resistance ◽  
Anticancer Agents ◽  
Rational Design ◽  
Genetic Diseases ◽  
Short Review ◽  
New Drugs ◽  
Anticancer Activities ◽  
Naturally Occurring ◽  
Body Tissues ◽  
Privileged Structures

: Cancers, a set of genetic diseases that can change the behavior and cell growth in body tissues, are the second leading cause of death accross the world. Several treatment approaches such as radiation, immunotherapy and chemotherapy can be applied to cure cancer, and among them, chemotherapy is one of the primary treatments for cancer, in which chemotherapeutic drugs are used. Great achievements have been made in the development of novel anticancer agents, but drug resistance is usually generated quickly, making overcoming drug resistance or developing more effective anticancer agents an imperative challenge. β-Lactones (2-oxetanones) are chemically diverse and often referred as privileged structures for the discovery of new drugs including anticancer agents. Marizomib (Salinosporamide A), a naturally occurring β-lactone proteasome inhibitor derived from the marine actinobacterium Salinispora tropica, has been termed as orphan drug against multiple myeloma. Therefore, β-lactones are useful scaffolds for the discovery of novel anticancer agents. This review is an endeavour to highlight the advances in β-lactone derivatives with anticancer potential, and the synthetic strategies, structure-activity relationships as well as modes of action are also discussed to pave the way for further rational design.

Morphological Characteristics of the Stroma in Malignat Epithelial Neoplasms with Short Review of Skin Squamous Cell Carcinoma

2014 ◽  
Vol 68 (1) ◽  
pp. 8-15
Author(s):  
Lena Kakasheva-Mazhenkovska ◽  
Vesna Janevska ◽  
Gordana Petrushevska ◽  
Liljana Spasevska ◽  
Neli Basheska
Keyword(s):  
Immune Cells ◽  
Complex Structure ◽  
Tumor Development ◽  
Morphological Characteristics ◽  
Basal Membrane ◽  
Short Review ◽  
Invasion And Metastasis ◽  
Genetic Changes ◽  
Cancer Associated Fibroblast ◽  
Skin Squamous Cell Carcinoma

Abstract The stroma of the neoplasm is a highly complex structure built by: specialized mesenchymal cells typical for each tissue surroundings, cancer associated fibroblast/myofibroblast, congenital or acquired immune cells, vascular network with endothelial cells and pericytes, mastocytes, macrophages, leukocytes and adipocytes, all together incorporated in the extracellular matrix. Each neoplasm produces its own unique microenvironment where the tumor grows and modifies. Although most of the cells of the host in the stroma have compulsory tumor suppressor ability, the stroma is changing during the malignant process and it even promotes growth, invasion and metastasis. Genetic changes that occur during the development of the cancer, which are guided by the malignant cells lead to changes in the stroma of the host that will overtake it and adjust it to their own needs. In the early stages of the tumor development and invasion, the basal membrane is degraded and the stroma becomes active and contains an increased number of fibroblasts, inflammatory infiltrate and newly composed capillaries which come into direct contact with the tumor cells. These changes lead to cancer invasion.

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.

Current insights into the chemistry and antitubercular potential of benzimidazole and imidazole derivatives

2020 ◽  
Vol 20 ◽  
Author(s):  
Deepa Parwani ◽  
Sushanta Bhattacharya ◽  
Akash Rathore ◽  
Chaitali Mallick ◽  
Vivek Asati ◽  
...  
Keyword(s):  
Drug Resistance ◽  
Mycobacterium Tuberculosis ◽  
Multi Drug Resistance ◽  
Benzimidazole Derivatives ◽  
Duration Of Treatment ◽  
Structure Activity ◽  
Mdr Tb ◽  
Low Toxicity ◽  
Extensively Drug Resistance ◽  
Improved Characteristics

: Tuberculosis is a disease caused by Mycobacterium tuberculosis (Mtb), affecting millions of people worldwide. The emergence of drug resistance is a major problem in the successful treatment of tuberculosis. Due to the commencement of MDR-TB (multi-drug resistance) and XDR-TB (extensively drug resistance), there is a crucial need for the development of novel anti-tubercular agents with improved characteristics such as low toxicity, enhanced inhibitory activity and short duration of treatment. In this direction, various heterocyclic compounds have been synthesized and screened against Mycobacterium tuberculosis. Among them, benzimidazole and imidazole containing derivatives found to have potential anti-tubercular activity. The present review focuses on various imidazole and benzimidazole derivatives (from 2015-2019) with their structure activity relationships in the treatment of tuberculosis.

Sign in / Sign up

Export Citation Format

Share Document