Use of Fluorine in the Medicinal Chemistry and Chemical Biology of Bioactive Compounds-A Case Study on Fluorinated Taxane Anticancer Agents

ChemBioChem ◽  
2004 ◽  
Vol 5 (5) ◽  
pp. 628-635 ◽  
Author(s):  
Iwao Ojima
Keyword(s):  
Bioactive Compounds ◽  
Anticancer Agents ◽  
Chemical Biology ◽  
Medicinal Chemistry

scholarly journals MW-Assisted Synthesis of Eight New 6-Nitrilmethyl Pyrrolo[3,4-b]pyridin-5-Ones via a Domino Process: aza Diels–Alder/N-Acylation/Aromatization

Proceedings ◽  
2018 ◽  
Vol 9 (1) ◽  
pp. 5 ◽  
Author(s):  
Manuel A. Rentería-Gómez ◽  
Shrikant G. Pharande ◽  
Alejandro Islas-Jácome ◽  
Eduardo González-Zamora ◽  
Rocío Gámez-Montaño
Keyword(s):  
Maleic Anhydride ◽  
Heat Source ◽  
Bioactive Compounds ◽  
Anticancer Agents ◽  
Medicinal Chemistry ◽  
Diels Alder ◽  
Experimental Procedure ◽  
The Core ◽  
Molecular Complexity ◽  
Chemistry Community

An efficient Microwave (MW)-assisted synthesis of eight new 6-nitrilmethyl-pyrrolo[3,4-b]pyridin-5-ones via a domino process: aza Diels–Alder/N-acylation/aromatization (dehydration–decarboxylation) from their corresponding 2-aminonitrile-oxazoles and maleic anhydride are described. The use of MW as a heat source and scandium (III) triflate as a catalyst to promote the cycloaddition process was crucial to construct these polyfunctionalized products in very good yields (51–79%), considering both their molecular complexity and that only one domino-type experimental procedure was required for their synthesis. It is worth noting that all products reported herein have not been synthesized nor isolated anywhere. However, they can be of high interest for the synthetic and medicinal chemistry community because pyrrolo[3,4-b]pyridin-5-one is the structural core of various bioactive compounds. In the same context, it can be considered as a privileged aza analogue of the isoindolin-1-one, which in turn is the core of numerous anticancer agents.

Novel Chemotherapeutic Agents - The Contribution of Scorpionates

2020 ◽  
Vol 26 (41) ◽  
pp. 7452-7475 ◽  
Author(s):  
Marta A. Andrade ◽  
Luísa M.D.R.S. Martins
Keyword(s):  
Transition Metal ◽  
Metal Complexes ◽  
Transition Metal Complexes ◽  
Anticancer Agents ◽  
Medicinal Chemistry ◽  
Bioinorganic Chemistry ◽  
Chemotherapeutic Agents ◽  
Great Role ◽  
Anticancer Properties ◽  
Scorpionate Ligands

: The development of safe and effective chemotherapeutic agents is one of the uppermost priorities and challenges of medicinal chemistry and new transition metal complexes are being continuously designed and tested as anticancer agents. Scorpionate ligands have played a great role in coordination chemistry, since their discovery by Trofimenko in the late 1960s, with significant contributions in the fields of catalysis and bioinorganic chemistry. Scorpionate metal complexes have also shown interesting anticancer properties, and herein, the most recent (last decade) and relevant scorpionate complexes reported for application in medicinal chemistry as chemotherapeutic agents are reviewed. The current progress on the anticancer properties of transition metal complexes bearing homo- or hetero- scorpionate ligands, derived from bis- or tris-(pyrazol-1-yl)-borate or -methane moieties is highlighted.

scholarly journals Food Bioactive Compounds and Emerging Techniques for Their Extraction: Polyphenols as a Case Study

Foods ◽  
2020 ◽  
Vol 10 (1) ◽  
pp. 37 ◽  
Author(s):  
José S. Câmara ◽  
Bianca R. Albuquerque ◽  
Joselin Aguiar ◽  
Rúbia C. G. Corrêa ◽  
João L. Gonçalves ◽  
...  
Keyword(s):  
Bioactive Compounds ◽  
Chemical Structure ◽  
Experimental Studies ◽  
Analytical Techniques ◽  
Convincing Evidence ◽  
Protective Effects ◽  
Extraction Techniques ◽  
Biological Impact ◽  
Preventive Effects

Experimental studies have provided convincing evidence that food bioactive compounds (FBCs) have a positive biological impact on human health, exerting protective effects against non-communicable diseases (NCD) including cancer and cardiovascular (CVDs), metabolic, and neurodegenerative disorders (NDDs). These benefits have been associated with the presence of secondary metabolites, namely polyphenols, glucosinolates, carotenoids, terpenoids, alkaloids, saponins, vitamins, and fibres, among others, derived from their antioxidant, antiatherogenic, anti-inflammatory, antimicrobial, antithrombotic, cardioprotective, and vasodilator properties. Polyphenols as one of the most abundant classes of bioactive compounds present in plant-based foods emerge as a promising approach for the development of efficacious preventive agents against NCDs with reduced side effects. The aim of this review is to present comprehensive and deep insights into the potential of polyphenols, from their chemical structure classification and biosynthesis to preventive effects on NCDs, namely cancer, CVDs, and NDDS. The challenge of polyphenols bioavailability and bioaccessibility will be explored in addition to useful industrial and environmental applications. Advanced and emerging extraction techniques will be highlighted and the high-resolution analytical techniques used for FBCs characterization, identification, and quantification will be considered.

Recent Advances on Small Molecule Medicinal Chemistry to Treat Human Diseases-Part III

2021 ◽  
Vol 21 (17) ◽  
pp. 1517-1518
Author(s):  
Dharmendra Kumar Yadav
Keyword(s):  
Natural Products ◽  
Drug Discovery ◽  
Small Molecule ◽  
Anticancer Agents ◽  
Medicinal Chemistry ◽  
Review Article ◽  
Human Diseases ◽  
Bioactive Metabolite ◽  
Metabolite Production ◽  
Life Threatening

The discovery and utilization of novel metabolites from natural sources are gaining momentum in the present era. The drug discovery programs have witnessed a remarkable shift from conventional medicines to exploiting natural products and their “value addition”, for treating lifethreatening diseases. The global outbreak of life-threatening diseases namely Ebola, SARS,including infections of the bloodstream (bacteremia), heart valves (endocarditis), lungs (pneumonia), and brain (meningitis) and AIDS calls for a more targeted approach to effectively combat the emerging diseases. In the present scenario, natural products and their extracts are being explored extensively for the treatment of various life threatening diseases. In this thematic issue, several review articles contributed by the scientist and researchers in the different areas of medicinal chemistry, synthetic chemistry, new emerging multi-drug targets were collected. This issue begins with a review article on the “Chemistry and Pharmacology of Natural Catechins from Camellia sinensis as anti-MRSA agents” by Gaur et al. and focuses on the spread of MRSA strains is of great concern because of limited treatment options for staphylococcal infections, since these strains are resistant to the entire class of β-lactam antibiotics. In addition, MRSA exhibits resistance to other classes of antimicrobial agents such as fluoroquinolones, cephalosporins, aminoglycosides, macrolide and even glycopeptides (vancomycin and teicoplanine), leading to the emergence of resistant strains such as glycopeptide intermediate (GISA) and resistant strain (GRSA) of S. aureus. In this review, chemical constituents responsible for the anti-MRSA activity of tea are explored [1]. The next article of this issue is a review article on the “Recent Advancements in the Synthesis and Chemistry of Benzofused Nitrogen- and Oxygen-based Bioactive Heterocycles” by Sharma et al. which focuses on medicinal importance of these bioactive benzo-fused heterocycles; special attention has been given to their synthesis as well as medicinal/pharmaceutical properties in detail [2]. “Trends in pharmaceutical design of Endophytes as anti-infective,” by Tiwari et al., is the third article in this issue. The review focused on the meta-analysis of bioactive metabolite production from endophytes, extensively discussing the bioprospection of natural products for pharmaceutical applications. In light of the emerging importance of endophytes as antiinfective agents, an exploration of the pharmaceutical design of novel chemical entities and analogues has enabled efficient and cost-effective drug discovery programs. However, bottlenecks in endophytic biology and research requires a better understanding of endophytic dynamics and mechanism of bioactive metabolite production towards a sustainable drug discovery program [3]. The last article of this issue is also research article on “Recent development of tetrahydro-quinoline/isoquinoline based compounds as anticancer agents” by Yadav et al. The article reported the synthesis of potent tetrahydroquinoline/isoquinoline molecules of the last 10 years with their anticancer properties in various cancer cell lines and stated their half-maximal inhibitory concentration (IC50). In addition, we also considered the discussion of molecular docking and structural activity relationship wherever provided to understand the possible mode of activity an target involved and structural features responsible for the better activity, so the reader can directly find detail for designing new anticancer agents. [4]. Finally I would like to thank all authors who contributed to this issue, titled “Recent advances on small molecule medicinal chemistry to treat human diseases”.

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