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Glycyrrhiza glabra (Licorice) and Gymnema sylvestre (Gurmar)
Published in Azamal Husen, Herbs, Shrubs, and Trees of Potential Medicinal Benefits, 2022
Jasbir Kaur, Sana Nafees, Mohd Anwar, Jamal Akhtar, Nighat Anjum
Antiviral: Glycyrrhizin works by preventing the viral cell from binding to the receptor. Recently, the antiviral effects of glycyrrhizin, ribavirin, mycophenolic acid, 6-azauridine, and pyrazofurin were evaluated against two clinical isolates of the severe acute respiratory syndrome virus (SARS), namely FFM-1 and FFM-2 (Badam 1997). Glycyrrhizin is considered to be the most effective way to control viral replication and can be used as a preventative measure. Previously, glycyrrhizin has been reported in hepatitis C virus and HIV-1 virus (De Clercq, 2000).
Cellular Oncogenes as Biotherapeutic Targets for the Differentiation and Inhibition of Cancer Cells
Published in Robert I. Glazer, Developments in Cancer Chemotherapy, 2019
Robert I. Glazer, Angelo Aquino, Gang Yu
Apart from the more commonly used differentiating agents such as DMSO, TPA, l,25(OH)2D3, and retinoic acid, a diverse spectrum of other compounds elicits morphologic changes in HL-60 cells.1 In general, the more cytotoxic the drug, the less differentiation occurs, and the narrower the dose-response relationship. Antimetabolite drugs such as the nucleoside analogs 5-azacytidine37 and neplanocin A (Figure 1),38,39 which preferentially inhibit the methylation of DNA and RNA respectively, induce a partial differentiation response in HL-60 cells mainly because of their potent cytocidal activities (Figure 2). Cell cycle specificity also plays a role in differentiation. The agents DMSO and retinoic acid generally produce an accumulation of cells in the G0/G1 phase of the cell cycle,40,41 an event which accompanies or precedes differentiation. The cytidine analog cyclopentenyl cytidine (CTP) (Figure 1) produces a rapid induction of mature myeloid cells upon treatment of HL-60 cells due to its ability to inhibit CTP synthesis, rapidly inhibit DNA synthesis, and inhibit cells from traversing S phase (Figure 2).42,43 The latter effect on HL-60 cells is also expressed by other inhibitors of CTP synthetase such as carbodine42 and 3-deazauridine,44 and by pyrazofurin, an inhibitor of orotidylate decarboxylase.44 Drugs which inhibit purine synthesis de novo such as the IMP dehydrogenase inhibitors tiazofurin and mycophenolic acid appear to be less effective inducers of myeloid differentiation in HL-60 cells.44,45
Synthesis, in silico modelling, and in vitro biological evaluation of substituted pyrazole derivatives as potential anti-skin cancer, anti-tyrosinase, and antioxidant agents
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2023
Samuel T. Boateng, Tithi Roy, Kara Torrey, Uchechi Owunna, Sergette Banang-Mbeumi, David Basnet, Eleonora Niedda, Alexis D. Alexander, Denzel El Hage, Siriki Atchimnaidu, Bolni Marius Nagalo, Dinesh Aryal, Ann Findley, Navindra P. Seeram, Tatiana Efimova, Mario Sechi, Ronald A. Hill, Hang Ma, Jean Christopher Chamcheu, Siva Murru
Numerous small-molecule compounds incorporating a pyrazole substructure exhibit one or more biological activities among a wide array thereof. Of medicinal relevance, these activities include analgesic, anticancer, antibacterial, antifungal, anti-inflammatory, antiviral, antidiabetic, antitubercular, antidepressant, anticonvulsant, antipyretic, anxiolytic, antimalarial, immunosuppressive, and antioxidant (reviewed in refs.60–67) The large number of structurally diverse compounds elaborated from a pyrazole core includes representatives exhibiting anticancer activities of wide-ranging character and demonstrated or apparent efficacies against cancers appearing in almost every human organ or tissue, including lung, brain, colon, kidney, prostate, pancreas, and blood68,69. Exemplary market-approved pyrazole-based anti-cancer drugs include crizotinib, encorafenib, pyrazofurin, and tartrazine. Various other pyrazole and pyrazolone derivatives have also exhibited antiproliferative activities mediated through their interactions with various cancer related targets, or directly (Figure 1)65,70–75.
Design, synthesis, molecular modelling and biological evaluation of novel 3-(2-naphthyl)-1-phenyl-1H-pyrazole derivatives as potent antioxidants and 15-Lipoxygenase inhibitors
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2020
Sahar A. Ali, Samir Mohamed Awad, Ahmed Mohammed Said, Shahenda Mahgoub, Heba Taha, Naglaa Mohamed Ahmed
Pyrazole ring is an important scaffold in medicinal chemistry. Pyrazole is a five-membered heterocyclic ring that consists of three carbons and two adjacent nitrogen atoms. Pyrazole derivatives have received considerable attention due to their remarkable broad spectrum of medicinal and pharmacological activities i.e. anticancer9, antiviral10, anti‐tubercular11, anti-microbial12, antimalarial13, anti-inflammatory14, antihypertensive15, anti-Alzheimer’s16, antipsychotic17, and antiparkinsonian18. Various drugs that have pyrazole ring are available in the market with diverse medicinal activities i.e. celecoxib I as anti-inflammatory19, Crizotinib II as anticancer20, Apixaban III as anticoagulant21, Pyrazofurin IV as anticancer, antibiotic22 and Fezolamine V as antidepressant23 (Figure 1).
The emergence of dihydroorotate dehydrogenase (DHODH) as a therapeutic target in acute myeloid leukemia
Published in Expert Opinion on Therapeutic Targets, 2018
Historically, the use of small molecule inhibitors of DNA and RNA synthesis is common in cancer chemotherapy, and we have decades of experience with effective molecules such as 5-Fluorouracil, cytarabine, and methotrexate. Given the essential role of uridine monophosphate (UMP) in DNA and RNA synthesis, it is no surprise that multiple inhibitors of de novo pyrimidine synthesis have been identified as hits during in vitro cancer cell line screening efforts through the 1970s and 1980s. Indeed, inhibitors at every step of pyrimidine synthesis have been studied in clinical trials; N-(phosphonacetyl)-L-aspartate (PALA) as an inhibitor of the aspartate-transcarbamylase function of CAD, brequinar sodium as an inhibitor of DHODH, and pyrazofurin as an inhibitor of the orotate-phosphoribosyltransferase function of UMPS (Figure 1).