ChemInform Abstract: Synthesis of Polyketide Natural Products and Analogues as Promising Anticancer Agents

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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Anticancer Agents from Diverse Natural Sources

Natural Product Communications ◽

10.1177/1934578x1400901130 ◽

2014 ◽

Vol 9 (11) ◽

pp. 1934578X1400901 ◽

Cited By ~ 8

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.

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POTENTIAL NATURAL PRODUCTS WITH ANTICANCER PROPERTIES AND THEIR APPLICATIONS

Asian Journal of Pharmaceutical and Clinical Research ◽

10.22159/ajpcr.2019.v12i5.32817 ◽

2019 ◽

pp. 27-33 ◽

Cited By ~ 1

Author(s):

BALABHASKAR R ◽

RAJENDRA KUMAR A ◽

SELVARAJAN S ◽

FARIDHA A ◽

GAYATHRI GUNALAN

Keyword(s):

Natural Products ◽

Anticancer Agents ◽

World Population ◽

Aromatic Plants ◽

Medicinal And Aromatic Plants ◽

Chemopreventive Agents ◽

Anticancer Properties ◽

Drug Molecules ◽

Animal Resources ◽

Drug Leads

Natural products continue to be a source for the discovery of drugs and drug leads even from ancient period. 80% of drug molecules have been obtained from either natural products or derivatives of the natural product. It has been found that the concept of a single drug for treating single disease may become outdated in the near future and the need of polyherbal formulations, as an alternate remedy is under investigation. Medicinal and aromatic plants contain biologically important phytochemicals, which have known curative properties. They are found as secondary metabolites in plants. Plants also contain certain other compounds that moderate the effects of the active ingredients. Medicinal and aromatic plants have their own contribution toward the treatment of both noncommunicable and communicable diseases. A survey done by the WHO indicates that a majority of the world population tends to use plants for treating diseases. Cancer, the second largest cause of death after cardiovascular disease accounts for about 3500 million people globally. Due to the serious side effects of synthetic chemopreventive agents, research is going onto investigate the nature derived chemopreventive agents. In addition to the plant-derived compounds, marine, and animal resources also play an important role as clinically beneficial anticancer agents with minimal or no toxicity. The best examples for plant-derived compounds include vincristine, vinblastine, irinotecan, etoposide, and paclitaxel; they have a different mode of action against cancer such as interaction with microtubules, inhibition of topoisomerases I or II, alkylation of DNA, and interference with tumor signal transduction. The natural products from marine sources such as bryostatin, squalamine exhibit a significant antimitotic, and anti-angiogenic activities. The benefits of various anticancer drugs derived from natural products are the fact that it can have its effect on cancer cells alone without harming healthy cells, which is unlikely to be the case with other conventional chemotherapeutics. In this review, various natural products and their anticancer properties have been discussed briefly.

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Anticancer Agents from Natural Products. Herausgegeben von Gordon M. Cragg, David G. I. Kingston und David J. Newman.

Angewandte Chemie ◽

10.1002/ange.200585390 ◽

2006 ◽

Vol 118 (38) ◽

pp. 6396-6397

Author(s):

Karl-Heinz Altmann

Keyword(s):

Natural Products ◽

Anticancer Agents

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Biodiversity as a source of new pharmacophores: A new theory of memory III

Pure and Applied Chemistry ◽

10.1351/pac200577010075 ◽

2005 ◽

Vol 77 (1) ◽

pp. 75-81 ◽

Cited By ~ 6

Author(s):

◽

M. Iqbal Choudhary

Keyword(s):

Natural Products ◽

Anticancer Agents ◽

Neurological Disorders ◽

In Vitro Bioassay ◽

Natural Sources ◽

Chemical Basis ◽

Antioxidant Agents ◽

A Cell ◽

The Brain

Several classes of natural products with significant inhibitory activity against target enzymes involved in several diseases have been identified. Spectrophotometer and high-throughput assays were used to assess the inhibition of prolyl endopeptidase (PEP), which led us to some novel inhibitors having potential as anticancer agents. Inhibition of cholinesterase enzymes has led to the discovery of new inhibitors with potential for use in Alzheimer’s disease and other neurological disorders. We have also discovered several potent antioxidant agents from natural sources by using a battery of antioxidant assays. Anti-inflammatory activity of a number of natural products was assayed through a cell-based in vitro bioassay. This article also contains a section on a slightly different topic of chemical basis of memory as presented during the lecture. The theory of the chemical basis of memory based on hydrogen bonding in the brain is further elaborated.

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