scholarly journals Strategies for the synthesis of brevipolides

2021 ◽  
Vol 17 ◽  
pp. 2399-2416
Author(s):  
Yudhi Dwi Kurniawan ◽  
A'liyatur Rosyidah
Keyword(s):  
Invasive Plant ◽  
Furan Ring ◽  
Human Cancer ◽  
Biological Activities ◽  
Structural Features ◽  
Review Article ◽  
Human Cancer Cell Lines ◽  
Chemokine Receptor Ccr5 ◽  
Synthetic Methodologies ◽  
Receptor Ccr5

In recent years fifteen 5,6-dihydro-α-pyrone derivatives, bearing either a distinctive cyclopropane or furan ring and named brevipolides A–O (1–15), have been isolated from the invasive plant Hyptis brevipes Poit. Their fascinating structural features, and the potent biological activities, including cytotoxicity against an array of human cancer cell lines and inhibition of the chemokine receptor CCR5, make them attractive synthetic targets. This review article highlights the recent synthetic methodologies and briefly summarizes their biological activities.

scholarly journals Biological Activity and Chemical Constituents of Essential Oil and Extracts of Murraya microphylla

2015 ◽  
Vol 10 (9) ◽  
pp. 1934578X1501000
Author(s):  
Hai-Ning Lv ◽  
Ke-Wu Zeng ◽  
Bing-Yu Liu ◽  
Yun Zhang ◽  
Peng-Fei Tu ◽  
...  
Keyword(s):  
Essential Oil ◽  
Human Cancer ◽  
Biological Activities ◽  
Chemical Constituents ◽  
Cytotoxic Activities ◽  
Active Components ◽  
Human Cancer Cell Lines ◽  
Total Oil ◽  
Promising Development ◽  
Carbazole Alkaloids

Murraya microphylla is the most closely related species to M. koenigii (Curry tree). Inspired by the traditional effects of M. koenigii, the antioxidant, anti-inflammatory, and cytotoxic activities of the essential oil and extracts of M. microphylla were evaluated for the first time. The light petroleum and chloroform extracts were found to be able to scavenge DPPH free radicals, inhibit linoleic acid peroxidation, and nitric oxide production, as well as to present cytotoxicity to the human cancer cell lines HepG2, Bel7402, Bel7403, and Hela, but the essential oil only showed moderate activities. Chemical analysis of the active extracts by LC-DAD-MSn indicated that carbazole alkaloids were the main constituents. GC-MS analysis of the essential oil resulted in identification of 91 constituents, representing 96.9% of the total oil, with ( E)-caryophyllene (18.4%) and terpinen-4-ol (12.6%) as the major constituents. These results demonstrate that M. microphylla has similar biological activities, as well as chemical constituents to M. koenigii, and the carbazole alkaloids were disclosed to be the main potential active components. A promising development as a flavor and potential therapeutic agent could thus be predicated for this plant.

scholarly journals An Updated Review on Synthesis and Biological Activities of Thiosemicarbazide Analogs

2021 ◽  
Vol 33 (9) ◽  
pp. 1957-1975
Author(s):  
Akhalesh Kumar ◽  
Rakhi Mishra ◽  
Avijit Mazumder ◽  
Rupa Mazumder ◽  
Arun Kumar
Keyword(s):  
Drug Discovery ◽  
Review Paper ◽  
Biological Activities ◽  
Reaction Scheme ◽  
Review Article ◽  
Pharmacological Activities ◽  
Thiosemicarbazide Derivative ◽  
Synthetic Methodologies ◽  
Thiosemicarbazide Derivatives

This review paper focuses on the different synthetic methodologies that researchers have adopted to synthesize various thiosemicarbazide derivatives with different biological activities of synthesized compounds in the last 20 years. Most of the investigations available in the literature are directed to the biological activities of thiosemicarbazide derivatives with less discussion on its synthetic schemes. This review article presents various reaction scheme, which has been adopted for thiosemicarbazide derivative synthesis along with the reported pharmacological activities of synthesized analogs. The available literature in the article aims to encourage more studies on the synthesis of thiosemicarbazide derivatives, which will help for drug discovery having thiosemicarbazide nucleus.

scholarly journals Phytohormones as Potential Anticancer Agents

2021 ◽  
Vol 8 (3) ◽  
Author(s):  
Ashmit Gill ◽  
Somi Patranabis
Keyword(s):  
Anticancer Agents ◽  
Human Cancer ◽  
Medical Problem ◽  
Review Article ◽  
Global Burden ◽  
Growth And Survival ◽  
Human Cancer Cell Lines ◽  
Current State ◽  
Naturally Occurring ◽  
Growth Development

The global burden of cancer is projected to have more than doubled over the next two decades, raising the prospect of a significant investment in health systems, thus posing a real medical problem. The increasing number of people with cancer highlights the need for more cancer prevention efforts. An established history exists for plant-derived compounds as effective anticancer agents. More recently, several phytohormones have been assessed for their ability to inhibit the growth and survival of human cancer cell lines. Phytohormones or plant hormones are chemical messengers responsible for harmonizing various cellular activities that revolves around growth, development, and stress-response. The aim of this literature review article is to present the current state of knowledge concerning the several naturally occurring phytohormones which have shown enormous potential in the prevention and treatment of variety of different type of cancers.

Cytotoxicity and Anti-cancer Activity of the Genus Achillea L.

2020 ◽  
Vol 27 (41) ◽  
pp. 6910-6925 ◽  
Author(s):  
Konstantina Papakosta ◽  
Maria-Eleni Grafakou ◽  
Christina Barda ◽  
Ioannis V. Kostopoulos ◽  
Ourania Tsitsilonis ◽  
...  
Keyword(s):  
Secondary Metabolites ◽  
Traditional Medicine ◽  
Human Cancer ◽  
Biological Activities ◽  
Northern Greece ◽  
Human Cancer Cell Lines ◽  
Anti Cancer ◽  
Analgesic Agents ◽  
Selection Of

Background: The genus Achillea L. is rich in bioactive sesquiterpenes and flavonoids; most of the studied species exhibit several biological activities and are used as emmenagogue, wound healing and analgesic agents. Some species are also used in local folklore medicine. Objective: Following a literature survey, we discuss the anti-cancer properties of Achillea species, taking into consideration ethnopharmacological data on their use in traditional medicine for the treatment of cancer. In addition, we screened extracts and isolated secondary metabolites from A. coarctata for cytotoxicity, upon information based on local traditional medicine. The plant was collected in Kozani (Northern Greece), where it is locally used for treating gastrointestinal disorders, including stomach cancer. Methods: A selection of the relevant data was performed through a search in PubMed, Scopus, Google Scholar and Science Direct databases. In addition, extracts and isolated compounds from A. coarctata were tested for their in vitro activity against the human cancer cell lines MCF-7 and HeLa. Conclusion: The genus Achillea L. is a valuable source of bioactive secondary metabolites. The most significant outcome of the investigation of medicinal plants is the documentation and the assessment of the traditional information and its use and perspectives in the light of modern pharmacology.

scholarly journals Terpenoids from Glechoma hederacea var. longituba and Their Biological Activities

2022 ◽  
Author(s):  
Dong Hyun Kim ◽  
Zahra Khan ◽  
Sun Yeou Kim ◽  
Sang Un Choi ◽  
Chung Sub Kim ◽  
...  
Keyword(s):  
Cytotoxic Activity ◽  
Cell Lines ◽  
Human Cancer ◽  
Biological Activities ◽  
2D Nmr ◽  
C6 Glioma Cells ◽  
No Production ◽  
M Cell ◽  
Human Cancer Cell Lines ◽  
Glechoma Hederacea

Glechoma hederacea var. longituba (common name: ground-ivy) has been used for the treatment of asthma, bronchitis, cholelithiasis, colds, and inflammation. In the present study, three new sesquiterpene glycosides (1–3), two new diterpene glycosides (4–5), and four known compounds (6–9) were isolated from its MeOH extract. Structure elucidation was performed for the five new compounds (1–5) using 1D and 2D NMR, HRESIMS, ECD calculation, and chemical methods. All the isolates (1–9) were assessed for their anti-neuroinflammatory activity on nitric oxide (NO) production in lipopolysaccharide (LPS)-activated BV-2 cells, nerve growth factor (NGF) secretion stimulation activity in C6 glioma cells, and cytotoxic activity against four human cancer cell lines (A549, SK-OV-3, SK-MEL-2, and HCT15). Compounds 2 and 5–7 exhibited inhibitory effects on NO production with IC50 values of 52.21, 47.90, 61.61, and 25.35 μM, respectively. Compound 5 also exhibited a significant stimulating effect on NGF secretion (122.77 ± 8.10%). Compound 9 showed potent cytotoxic activity against SK-OV-3 (IC50 3.76 μM) and SK-MEL-2 (IC50 1.48 μM) cell lines, while 7 displayed a strong cytotoxic activity against SK-MEL-2 (IC50 9.81 μM) cell line

scholarly journals Coumarin sulfonamide derivatives: An emerging class of therapeutic agents

2020 ◽  
Vol 26 (1) ◽  
pp. 46-59 ◽  
Author(s):  
Ali Irfan ◽  
Laila Rubab ◽  
Mishbah Ur Rehman ◽  
Rukhsana Anjum ◽  
Sami Ullah ◽  
...  
Keyword(s):  
Therapeutic Potential ◽  
Biological Activities ◽  
Wide Spectrum ◽  
Structural Features ◽  
Therapeutic Agents ◽  
Review Article ◽  
Structural Motif ◽  
Structure Activity ◽  
Anti Cancer ◽  
Novel Therapeutic

AbstractCoumarin sulfonamide is a heterocyclic pharmacophore and an important structural motif which is a core and integral part of different therapeutic scaffolds and analogues. Coumarin sulfonamides are privileged and pivotal templates which have a broad spectrum of applications in the fields of medicine, pharmacology and pharmaceutics. Coumarin sulfonamide exhibited versatile and myriad biomedical activities such as anti-bacterial, antiviral, antifungal, anti-inflammatory and anti-cancer. This review article focuses on the structural features of coumarin sulfonamide derivatives in the treatment of different lethal diseases on the basis of structure-activity relationships (SAR). The plethora of research cited in this review article summarizes and discusses the various substitutions around the coumarin sulfonamide nucleus which have provided a wide spectrum of biological activities and therapeutic potential that has proved attractive to many researchers looking to exploit the coumarin sulfonamide skeleton for drug discovery and the development of novel therapeutic agents.

scholarly journals Cellular Basis of Organotin(IV) Derivatives as Anticancer Metallodrugs: A Review

2021 ◽  
Vol 9 ◽  
Author(s):  
Sharifah Nadhira Syed Annuar ◽  
Nurul Farahana Kamaludin ◽  
Normah Awang ◽  
Kok Meng Chan
Keyword(s):  
Molecular Mechanisms ◽  
Antimicrobial Agents ◽  
Human Cancer ◽  
Synergistic Effects ◽  
Biological Activities ◽  
Human Cancer Cell Lines ◽  
Cycle Arrest ◽  
Ability To Act ◽  
Potential Applications ◽  
Anticancer Metallodrugs

Organotin(IV) compounds have wide applications in industrial and agricultural fields owing to their ability to act as poly(vinyl chloride) stabilizers and catalytic agents as well as their medicinal properties. Moreover, organotin(IV) compounds may have applications as antitumor, anti-inflammatory, antifungal, or antimicrobial agents based on the observation of synergistic effects following the binding of their respective ligands, resulting in the enhancement of their biological activities. In this review, we describe the antiproliferative activities of organotin(IV) compounds in various human cancer cell lines based on different types of ligands. We also discuss the molecular mechanisms through which organotin(IV) compounds induce cell death via apoptosis through the mitochondrial intrinsic pathway. Finally, we present the mechanisms of cell cycle arrest induced by organotin(IV) compounds. Our report provides a basis for studies of the antitumor activities of organotin(IV) compounds and highlights the potential applications of these compounds as anticancer metallodrugs with low toxicity and few side effects.

scholarly journals An Efficient, Three-Component Synthesis of Isoindolin-1-One-3-Phosphonates Under Mild and Solvent-Free Conditions and Their Biological Activities

2021 ◽  
Author(s):  
Hamida Jelali ◽  
Ibrahim S. Al Nasr ◽  
Waleed S. Koko ◽  
Tariq A. Khan ◽  
Eric Deniau ◽  
...  
Keyword(s):  
Leishmania Major ◽  
Human Cancer ◽  
Biological Activities ◽  
Antimicrobial Activities ◽  
Primary Amines ◽  
One Pot ◽  
Human Cancer Cell Lines ◽  
Solvent Free Conditions ◽  
Three Component Reaction

Abstract In this work, the synthesis of isoindolin-1-one-3-phosphonates by a ‘one-pot’ three-component reaction of 2-formylbenzoic acid with primary amines and dimethyl phosphite under solvent and catalyst free-conditions was reported. 1H NMR, 13C NMR, FT-IR and elemental analysis techniques, characterized the obtained compounds. The isoindolin-1-one-3-phosphonates were screened for their antimicrobial activities against bacteria and a fungus (Candida albicans). They were additionally also investigated for their anti-parasitical activities against Leishmania major promastigotes and amastigotes and Toxoplasma gondii in vitro. Cytotoxicity investigations of the isoindolin-1-one-3-phosphonates were led conducted in two human cancer cell lines, MDA-MB-231 and MCF-7and vero cells.

scholarly journals Design, Synthesis, and In Vitro Evaluation of Novel Indolyl DiHydropyrazole Derivatives as Potential Anticancer Agents

Molecules ◽  
2021 ◽  
Vol 26 (17) ◽  
pp. 5235
Author(s):  
Katharigatta N. Venugopala ◽  
Mohammed Habeebuddin ◽  
Bandar E. Aldhubiab ◽  
Afzal Haq Asif
Keyword(s):  
Anticancer Activity ◽  
Cell Lines ◽  
Anticancer Agents ◽  
Human Cancer ◽  
Structural Features ◽  
Synthetic Methods ◽  
Potential Candidate ◽  
Human Cancer Cell Lines ◽  
Hybrid Molecules

Indoles derived from both natural sources or artificial synthetic methods have been known to interact with aryl hydrocarbon receptors (AhR), and exhibit anticancer activity. In light of these attractive properties, a series of hybrid molecules with structural features of indoles, i.e., those bearing a pyrazoline nucleus, were evaluated for their enhanced anticancer activity. The designed molecules were subjected to molecular docking in order to screen for potential AhR interacting compounds, and the identified indolyl dihydropyrazole derivatives were synthesized. The synthesized compounds were characterized, and their cytotoxicity was evaluated against four human cancer cell lines using the MTT assay. Based on the Glide g-score, H-bonding interactions and bonding energy of 20 candidate molecules were selected for further analysis from the 64 initially designed molecules. These candidate molecules have shown promising anti-proliferative activity against the cell lines tested. Among these candidate molecules, the compounds with hydroxy phenyl substitution on the pyrazoline ring have shown potent activity across all the tested cell lines. The designed scaffold was proven effective for screening potential candidate molecules with anticancer properties, and may be further optimized structurally for yielding the ideal anti-tumorigenic compound for the treatment of various cancers.

Recent development of tetrahydro-quinoline/isoquinoline based compounds as anticancer agents

2021 ◽  
Vol 21 ◽  
Author(s):  
Pratik Yadav ◽  
Ashish Kumar ◽  
Ismail Althagafi ◽  
Vishal Nemaysh ◽  
Reeta Rai ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Anticancer Agents ◽  
Human Cancer ◽  
Biological Activities ◽  
Cancer Cell Lines ◽  
New Drugs ◽  
Anticancer Activities ◽  
Human Cancer Cell Lines ◽  
Anticancer Properties

: Tetrahydroquinoline and isoquinoline scaffolds are important class heterocyclic compounds, which is implied for the development of new drugs and diagnostic for therapeutic function. Naturally occurring as well as synthetic tetrahydroquinolines/isoquinolines possess many different biological activities and have been testified as remarkable cytotoxic and potency in human cancer cell lines. Tetrahydroquinoline/isoquinolines based compounds displayed a key role in the development of anticancer drugs or lead molecules and acting through various mechanisms such as cell proliferation, apoptosis, DNA fragmentation, inhibition of tubulin polymerization, induced cell cycle arrest, interruption of cell migration, and modulation. The number of tetrahydroquinoline/isoquinoline derivatives has been reported as potent anticancer agents. Due to promising anticancer activities and wide-ranging properties of these molecules, we have compiled the literature for the synthesis and anticancer properties of various tetrahydroquinolines and isoquinolines. We have 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 a target involved and structural feature responsible for the better activity, so the reader can directly find the detail for designing new anticancer agents.

Sign in / Sign up

Export Citation Format

Share Document