Oxazole-Based Compounds As Anticancer Agents

2020 ◽  
Vol 26 (41) ◽  
pp. 7337-7371 ◽  
Author(s):  
Maria A. Chiacchio ◽  
Giuseppe Lanza ◽  
Ugo Chiacchio ◽  
Salvatore V. Giofrè ◽  
Roberto Romeo ◽  
...  
Keyword(s):  
Cancer Research ◽  
Drug Discovery ◽  
Anticancer Agents ◽  
Heterocyclic Compounds ◽  
Chemical Diversity ◽  
Biologically Active ◽  
New Drugs ◽  
The Core ◽  
Anti Cancer ◽  
Biologically Active Derivatives

: Heterocyclic compounds represent a significant target for anti-cancer research and drug discovery, due to their structural and chemical diversity. Oxazoles, with oxygen and nitrogen atoms present in the core structure, enable various types of interactions with different enzymes and receptors, favoring the discovery of new drugs. Aim of this review is to describe the most recent reports on the use of oxazole-based compounds in anticancer research, with reference to the newly discovered iso/oxazole-based drugs, to their synthesis and to the evaluation of the most biologically active derivatives. The corresponding dehydrogenated derivatives, i.e. iso/oxazolines and iso/oxazolidines, are also reported.

Diverse thiophenes as scaffolds in anti-cancer drug development: A concise review

2020 ◽  
Vol 20 ◽  
Author(s):  
Neha V. Bhilare ◽  
Pratibha B. Auti ◽  
Vinayak S. Marulkar ◽  
Vilas J. Pise
Keyword(s):  
Drug Development ◽  
Anticancer Agents ◽  
Heterocyclic Ring ◽  
Biologically Active Compounds ◽  
Biologically Active ◽  
Cancer Drug ◽  
Active Compounds ◽  
Natural Origin ◽  
Concise Review ◽  
Anti Cancer

: Thiophenes are one among the abundantly found heterocyclic ring systems in many biologically active compounds. Moreover various substituted thiophenes exert numerous pharmacological actions on account of their isosteric resemblance with compounds of natural origin thus rendering them with diverse actions like antibacterial, antifungal, antiviral, anti-inflammatory, analgesic, antiallergic, hypotensives etc.. In this review we specifically explore the chemotherapeutic potential of variety of structures consisting of thiophene scaffolds as prospective anticancer agents.

Secondary Metabolites of Plant Origin containing Carbazole as Lead Molecule: A Review

2019 ◽  
Vol 05 ◽  
Author(s):  
Atul Sharma ◽  
Devender Pathak
Keyword(s):  
Drug Discovery ◽  
Heterocyclic Compounds ◽  
Biological Activities ◽  
Chemical Compounds ◽  
Lethal Effect ◽  
Chemical Diversity ◽  
Chemical Transformations ◽  
Pharmacological Effects ◽  
Structural Class ◽  
Biological Targets

Keeping this fact that study of a body is biology but life is all about chemicals and chemical transformations, many medicinal chemist start research in finding new and novel chemical compounds which having pharmacological activities. Most of those chemical compounds which are having active pharmacological effects are heterocyclic compounds. Heterocyclic compounds clutch a particular place among pharmaceutically active natural and synthetic compounds. The ability to serve both as biomimetics and reactive pharmacophores of heterocyclic nuclei is incredible and it has principally contributed to their unique value as traditional key elements of numerous drugs. These heterocyclic nuclei offer a huge area for new lead molecules for drug discovery and for generation of activity relationships with biological targets to enhance pharmacological effects. For these reasons, it is not surprising that this structural class has received special attention in drug discovery. The hydrogen bond acceptors and donors arranged in a manner of a semi-rigid skeleton in heterocyclic rings and therefore they can present a varied display of significant pharmacophores. Lead identification and optimization of drug target probable can be achieved by generation of chemical diversity produced by derivatization of heterocyclic pharmacophores with different groups or substituents. A tricyclic carbazole nucleus is an integral part of naturally occurring alkaloids and synthetic derivatives, possessing various potential biological activities such as anticancer, antimicrobial and antiviral. Binding mechanism of carbazole with target receptor as a molecule or fused molecule exhibits the potential lethal effect.

scholarly journals Anticancer Agents from Diverse Natural Sources

2014 ◽  
Vol 9 (11) ◽  
pp. 1934578X1400901 ◽  
Author(s):  
Jabeena Khazir ◽  
Darren L. Riley ◽  
Lynne A. Pilcher ◽  
Pieter De-Maayer ◽  
Bilal Ahmad Mir
Keyword(s):  
Clinical Trials ◽  
Natural Products ◽  
Anticancer Agents ◽  
Marine Organisms ◽  
New Drugs ◽  
Human Diseases ◽  
Cancer Drugs ◽  
Natural Sources ◽  
Anti Cancer ◽  
Ancient Times

This review attempts to portray the discovery and development of anticancer agents/drugs from diverse natural sources. Natural molecules from these natural sources including plants, microbes and marine organisms have been the basis of treatment of human diseases since the ancient times. Compounds derived from nature have been important sources of new drugs and also serve as templates for synthetic modification. Many successful anti-cancer drugs currently in use are naturally derived or their analogues and many more are under clinical trials. This review aims to highlight the invaluable role that natural products have played, and continue to play, in the discovery of anticancer agents.

Quinoline-based Compounds as Key Candidates to Tackle Drug Discovery Programs of Microbicidal Agents

2020 ◽  
Vol 26 ◽  
Author(s):  
Aline Nefertiti Silva da Gama ◽  
Maria de Nazaré Correia Soeiro
Keyword(s):  
Drug Discovery ◽  
Trypanosoma Brucei ◽  
Anticancer Agents ◽  
Biological Effect ◽  
Heterocyclic Compounds ◽  
Neglected Tropical Diseases ◽  
Pharmacological Properties ◽  
Tropical Diseases ◽  
Clinical Use ◽  
Leishmania Spp

: Quinolines are nitrogen heterocyclic compounds ubiquitous in nature and largely used as a structural component of dyes, solvent for resins, terpenes as well as during the production of several other chemical stuffs, including pesticides. Quinolines, such as quinine and chloroquine, exhibit various pharmacological properties, acting as antimalarial drugs, antiparasitic, antibacterial, antiviral, antifungal, and anticancer agents, besides being in clinical use for autoimmune diseases. Presently, a brief review is present regarding the biological effect and clinical use of quinolines and derivatives upon two trypanosomatids agents of important neglected tropical diseases; Trypanosoma cruzi, Trypanosoma brucei spp and Leishmania spp, which trigger Chagas disease, sleeping sickness and leishmaniasis, respectively, also extending to a glance update of their potential application towards other microbes relevant for emerging illness caused by fungi, bacteria and virus, including the pandemic Covid-19.

New Approaches for the Synthesis of Heterocyclic Compounds Corporating benzo[d]imidazole as Anticancer Agents, Tyrosine, Pim-1 Kinases Inhibitions and their PAINS Evaluations

2020 ◽  
Vol 20 ◽  
Author(s):  
Rafat M. Mohareb ◽  
Yara R. Milad ◽  
Bahaa M. Mostafa ◽  
Reem A. El-Ansary
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Anticancer Agents ◽  
Tyrosine Kinases ◽  
Heterocyclic Compounds ◽  
Cancer Cell Lines ◽  
Biologically Active ◽  
Strong Impact ◽  
Target Molecules

Background: Benzo[d]imidazoles are highly biologically active, in addition, they are considered as a class of heterocyclic compounds with many pharmaceutical applications. Objective: We are aiming in this work to synthesize target molecules not only possess anti-tumor activities but also kinase inhibitors. The target molecules were obtained starting from the benzo[d]imidazole derivatives followed by their heterocyclization reactions to produce anticancer target molecules. Methods: The 1-(1H-benzo[d]imidazol-2-yl)propan-2-one (3) and the ethyl 2-(1H-benzo[d]imidazol-2-yl)acetate (16) were used as the key starting material which reacted with salicylaldehyde to give the corresponding benzo[4,5]imidazo[1,2-a]quinoline derivatives. On the other hand, both of them were reacted with different reagents to give thiophene, pyran and benzo[4,5]imidazo[1,2-c]pyrimidine derivatives. The synthesized compounds were evaluated against the six cancer cell lines A549, HT-29, MKN-45, U87MG, and SMMC7721 and H460 together with inhibitions toward tyrosine kinases, c-Met kinase and prostate cancer cell line PC-3 were recorded using the standard MTT assay in vitro, with foretinib as the positive control. Results: Most of the synthesized compounds exhibited high inhibitions toward the tested cancer cell lines. In addition, tyrosine and Pim1 kinases inhibitions were performed for the most active compounds where variation of substituent through the aryl ring and heterocyclic ring afforded compounds with high activities. Our analysis showed that there is a strong correlation between structure of compound and substituents of target molecules. Conclusion: Our present research proved that the synthesized heterocyclic compounds with varieties of substituents has a strong impact through the activity of compounds. The evaluations through different cell lines and tyrosine kinases indicated that the compounds were excellent candidates as anticancer agents. This could encourage doing further research within this field for the building of compounds with high inhibitions.

THIAZOLES AS POTENT ANTICANCER AGENTS: A REVIEW

INDIAN DRUGS ◽  
2016 ◽  
Vol 53 (11) ◽  
pp. 5-11
Author(s):  
P. K. N Sarangi ◽  
◽  
J Sahoo ◽  
B. D. Swain ◽  
S. K. Paidesetty ◽  
...  
Keyword(s):  
Statistical Analysis ◽  
Anticancer Agents ◽  
Heterocyclic Compounds ◽  
Chemotherapeutic Agents ◽  
Thiazole Derivatives ◽  
Drug Molecules ◽  
Important Target ◽  
Rational Drug ◽  
Anti Cancer ◽  
Target Sites

The chemistry of heterocyclic compounds plays a crucial role in the synthesis of medicinals. This review focuses on the use of the thiazole nucleus for the synthesis of newer drug molecules through rational drug discovery. Here the synthetic feasibility, biochemical compatibility and the therapeutic utility of the thiazole derivatives is discussed briefly. Recently, it was observed that many chemotherapeutic agents have a thiazole nucleus. Hence, this article highlights the profound anti-cancer activities of some major thiazole bearing drug molecules with their important target sites. Along with this, the recent advancements in the development of thiazole based newer anti-cancer molecules and their promising activities are reviewed. The relevant data and some statistical analysis regarding the medicinal importance of thiazole nucleus will further promote the design and development of varieties of chemotherapeutic entities in the field of cancer treatment.

Bioinformatics approach on bioisosterism softwares to be used in drug discovery and development

2021 ◽  
Vol 16 ◽  
Author(s):  
Nelson José Freitas da Silveira ◽  
Walter Filgueira de Azevedo Jr. ◽  
Rita Cardoso Guedes ◽  
Leandro Marcos Santos ◽  
Rodolfo Cabral Marcelino ◽  
...  
Keyword(s):  
Drug Discovery ◽  
Mode Of Action ◽  
Wide Spectrum ◽  
Chemical Properties ◽  
Biologically Active Compounds ◽  
Biologically Active ◽  
New Drugs ◽  
Active Compounds ◽  
Research Areas ◽  
Reduced Toxicity

Background: In the rational drug development field, a bioisosterism is a tool that improves lead compounds performance, reffering to molecular fragment substitution that has similar physical-chemical properties. Thus, it is possible to modulate drug properties such as absorption, toxicity, and half-life increase. This modulation is of pivotal importance in the discovery, development, identification, and interpretation of the mode of action of biologically active compounds. Objective: Our purpose here is to review the development and application of bioisosterism in drug discovery. In this study history, applications, and use of bioisosteric molecules to create new drugs with high binding affinity in the protein-ligand complexes are described. Method: It is an approach for molecular modification of a prototype based on the replacement of molecular fragments with similar physicochemical properties, being related to the pharmacokinetic and pharmacodynamic phase, aiming at the optimization of the molecules. Results: Discovery, development, identification, and interpretation of the mode of action of biologically active compounds are the most important factors for drug design. The strategy adopted for the improvement of leading compounds is bioisosterism. Conclusion: Bioisosterism methodology is a great advance for obtaining new analogs to existing drugs, enabling the development of new drugs with reduced toxicity, in a comparative analysis with existing drugs. Bioisosterism has a wide spectrum to assist in several research areas.

Creating chemical diversity space by scaffold decoration of dihydropyrimidines

2005 ◽  
Vol 77 (1) ◽  
pp. 155-161 ◽  
Author(s):  
Doris Dallinger ◽  
C. Oliver Kappe
Keyword(s):  
Drug Discovery ◽  
Driving Force ◽  
New Technologies ◽  
Materials Science ◽  
Building Blocks ◽  
Chemical Diversity ◽  
Combinatorial Synthesis ◽  
Biologically Active ◽  
Compound Libraries

The demand for diverse compound libraries for screening in drug discovery and materials science is the driving force behind the development of new technologies for rapid parallel and combinatorial synthesis. The focus of this article will be on the scaffold decoration of biologically active dihydropyrimidines (DHPMs) of the Biginelli type, exploring the diversity on all six positions around the scaffold. This opens up the generation of a very large number of analogs given the commercial availability of the building blocks that are used in the functionalization process.

Sign in / Sign up

Export Citation Format

Share Document