2 edition of Synthesis of some anthrasteroids as potential anti-tumour agents found in the catalog.
Synthesis of some anthrasteroids as potential anti-tumour agents
Susie Seok Si Toh-Lewis
Written in English
Thesis (Ph.D.) - Loughborough University of Technology, 1993.
|Statement||by Susie Seok Si Toh-Lewis.|
-acne agents: benzoyl peroxide, erythromycin, tretinion (Retin-A)-antifungal (e.g. miconazole, clotrimozole)-used to treat candidiasis, dermatrophytes (tinea or athletes foot and jock itch)-antivirals used in treatment of herpes simplex 1 and 2 (inhibit viral enzymes necessary for DNA synthesis)-acyclovir, penciclovir. Farghaly AA, Bekhit AA, Park JY. Design and synthesis of some oxadiazolyl, thiazolidinyl and thiazolyl derivatives of 1H-pyrazole as anti-inflammatory and antimicrobial agents. Arch Pharm. ; –7.
[Nonsteroidal anti-inflammatory agents. Synthesis and activity of stereomeric phenylacetic homologues]. [Article in German] Varoli L(1), Burnelli S, Guarnieri A, Bonazzi D, Scapini G, Sarret M, Fantuz M. Author information: (1)Dipartimento di Scienze Farmaceutiche, Università di Bologna, Italia. Synthesis of compounds (1–4) Herein, we have synthesized four new ketoester deriva-tives of succinimides (1–4) by organocatalytic Michael additions of α-ketoesters to N-phenyl and N-benzyl mal-eimides. A number of available nitrogenous compounds were screened as achiral organocatalysts for the catalysis of these reactions.
Introduction. Prostate cancer is an androgen dependent malignancy, first demonstrated in by the Nobel Prize-winning research of Huggins and Hodges showing that reducing serum androgen levels by orchiectomy or exogenous estrogen administration induced tumor regressions and palliation of symptoms (Figure 1).Subsequently gonadotropin-releasing hormone (GnRH) analogs and antiandrogens were. The cytotoxic activity is due to cross-linking of DNA and RNA and DNA synthesis is inhibited. Side effects: Delayed myelosuppression (dose limiting), nausea/vomiting, stomatitis, alopecia, renal toxicity after longtime use. Indication: Curative as a single agent for choriocarcinoma, and in palliative treatment of various solid tumors.
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Synthesis of some anthrasteroids as potential anti-tumour agents This item was submitted to Loughborough University's Institutional Repository by the/an author.
Additional Information: • A Doctoral Thesis. Submitted in partial ful lment of the requirements for the award of Doctor of Philosophy of Loughborough Universit.y. Synthesis of some anthrasteroids as potential anti-tumour agents Selected hydroxylated anthrasteroids were designed to bind to the vitamin D receptors present in certain cancers, thereby inducing cell differentiation and inhibiting cell proliferation with reduction and/ or even elimination of the potent calcemic effects of vitamin D.
Total synthesis of anthrasteroids—I of the solvent gave 12'5 g (91 %) of IV as a colourless viscous oil. The UV spectrum of the crude material (EtOH): (e = ) nm indicated the presence of less than 5 % of the conjugated isomer10 and showed further no significant absorption, v'^, at,and cmCited by: 3.
As part of our investigations in the total synthesis of anthrasteroids we communicate in this paper the preparation of some 3-phenyl substituted 2,4-diaza-anthrasteroids.
As in our synthesis of anthraestrones and anthraequilenines,1 the tricyclic hydroxymethylene ketone, Cited by: 2. Synthesis of some novel androstanes as potential aromatase inhibitors Article in Steroids 76(5) April with 26 Reads How we measure 'reads'.
Synthesis, analysis and biological evaluation of novel indolquinonecryptolepine analogues as potential anti-tumour agents. Organic & Biomolecular Chemistry14 (11), DOI: /C5OBK.
Sébastien Comesse, Adam Daïch. This study revealed a new attractive cyclic-indole scaffold for the discovery of mitosis-targeting anti-tumour agents. Among all of the synthesized derivatives, compound 20 displayed the most potent anti-proliferative activity (with IC 50 values of 22–56 nM against seven cancer cell lines) and tubulin polymerization inhibition (IC 50 = ± μM), which were much better than those of.
Request PDF | Novel oxazine skeletons as potential antiplasmodial active ingredients: Synthesis, in vitro and in vivo biology of some oxazine entities produced via cyclization of novel chalcone.
N-(4-(Pyrazolyl)thiazolyl)-N′-phenylthiourea derivative 2 was synthesized and then treated with variety of hydrazonoyl chlorides under basic condition at reflux to afford the corresponding 2-(4-(pyrazolyl)thiazolylimino)-1,3,4-thiadiazole derivatives 6, 10a–e and 17a–on of 2 with ethyl chloroacetate and with 3-chloro-2,4-pentanedione gave the thiazolidinone 22 and.
Synthesis, biological evaluation and molecular docking of some substituted pyrazolines and isoxazolines as potential antimicrobial agents. Eur. Med. Chem. 95, 96– ().Crossref, Medline, CAS, Google Scholar; 45 He J, Ma L, Wei Z et al.
Synthesis and biological evaluation of novel pyrazoline derivatives as potent anti-inflammatory. 1. Introduction. The indole derivatives display a wide range of biological activities.
This is exemplified by the amino acid tryptophan, the hormones serotonin and melatonin, the anti-inflammatory drug indomethacin, the psychotropic drug LSD and the anti-tumour agent vinblastine. 1 Accordingly, the synthesis of indole derivatives has long been a topic of fundamental interest to organic and.
The acid‐catalyzed condensation of quinisatines 5a‐c or their aminals 4a‐c with phenols 6a‐i led to a number of 3‐hydroxy‐3‐hydroxyphenyl‐2,4‐dioxo‐1,2,3,4‐tetrahydroquinolines 7a‐s which were considered as potential antiinflammatory agents.
Some cyclization reactions with 4-thiohydantoin: Synthesis of some novel thiopyranoimidazoles, thienoimidazoles and imidazoquinolines and some metal complexes with biological interest Article Mar. Inhibitors of acyl-CoA:cholesterol acyltransferase: novel trisubstituted ureas as hypocholesterolemic agents.
Bioorganic & Medicinal Chemistry5 (4), DOI: /S(97) JY Nioche, J Decerprit, D Festal. Synthesis and structure-activity relationships of new ACAT inhibitors.
 In addition, several 1,3-thiazole scaffolds have been reported as potent anticancer agents.   The synthesis of some new pyrazole-based 1,3-thiazoles as anticancer agents. A convergent, stereocontrolled route to either antipode of the cell adhesion inhibitor, peribysin E, has been achieved from carvone.
Highlights of the synthesis include a Diels−Alder reaction to generate a cis-decalin framework, followed by semipinacol-type ring contraction to secure the stereochemistry of the C7 quaternary center. Potential mechanistic pathways for the critical ring.
Some of the target compounds showed good docking scores with potential anticancer targets, chosen based on pharmacophore mapping of the established derivatives. View Show abstract. The use of nonsteroidal anti-inflammatory drugs (NSAIDs) dates back to thousands of years when man used natural sources of these agents in a lot of pain and inflammatory conditions.
The tone for modern day discovery and use of NSAIDs was set with the discovery of aspirin. Today in addition to aspirin, a host of other NSAIDs of varying potency and efficacy is employed in the management of.
Endophytic fungi. Endophytic fungi are one of the major potential sources for the production of valuable bioactive compounds (Dreyfuss and Chapela ). Pestalotiopsis neglecta BAB, an endophytic fungus of Cupressus torulosa, is considered to be a promising source of phenols, flavonoids, terpenoids, alkaloids, tannins, carbohydrates and saponin (Sharma et al.
), while. This video explains about the #classification and mechanism of action of #antiarrhythmic_drugs / agents. Chapter 1: Cardiac Action Potential. Pederin is found in some beetles, e.g., Paederus fuscipes, and structurally is considered a polyketide that bears vesicant and potent antitumor properties.
Although pederin has weak antibacterial properties, it is severely toxic to eukaryotic cells. This property likely stems from its ability to block protein synthesis and cell division.What agents are among the most potent inhibitors of mast cell release.
β adrenergic. True or False 20 mg four times daily with the nebulizer solution in some cases can be reduced to a maintenance dosage of 40 to 60 mg per day after the patient is stabilized from 1 to 2 months. Some case‐control studies have linked the NSAIDs aspirin and indomethacin with a risk of congenital abnormalities and low birthweight.
High doses of aspirin produce developmental toxicity in rats (e.g., gastroschisis/umbilical hernia, diaphragmatic hernia [DH]) when administered during sensitive windows of development.