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2 edition of synthesis of "bioreversible" derivatives of the anti-tumour agent 2(superior)1-deoxy-5-fluorouridine. found in the catalog.

synthesis of "bioreversible" derivatives of the anti-tumour agent 2(superior)1-deoxy-5-fluorouridine.

Roger Neil Hunston

synthesis of "bioreversible" derivatives of the anti-tumour agent 2(superior)1-deoxy-5-fluorouridine.

by Roger Neil Hunston

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  • 35 Currently reading

Published by University of Birmingham in Birmingham .
Written in English


Edition Notes

Thesis (Ph.D.)-University of Birmingham, Dept of Chemistry.

ID Numbers
Open LibraryOL20661172M

Methods for the synthesis of N1, N8-bis(9-acridinyl)-N4-(4-hydroxybenzyl)-spermidine and N1, N7-(hydroxybenzyl)-bis-(3-aminopropyl)amine were investigated. Thus monocyanoethylation of 4-methoxybenzylamine followed by treatment with 4-chlorobutyronitrile gave the dinitrile N-(2-cyanoethyl)-N-(3-cyanopropyl)methoxybenzylamine. Subsequent in situ reduction with lithium aluminium Cited by:   Wang P, Xia Y-L, Yu Y et al. Design, synthesis and biological evaluation of esculetin derivatives as anti-tumour agents. RSC Adv. 5(66), – (). Crossref, Cited by: 3.

2, 3(Department of Chemistry, College of Education / University of Tikrit, Tikrit, Iraq) Abstract: This research, involved synthesis of a series of new compound containing different derivatives. The synthesis involved treatment of 6- methyl 2-thiouracil with chloroacetyl chloride to give 1- chloroacetyl 6-File Size: 1MB. carbothiaote derivatives were synthesized. Substituted 2-phenyl-benzothiazole were synthesised by condensing substituted benzoic acid with 2-amino thiophenol in the presence of phosphoric acid and 3-benzothiazoleylsubstituted carbothiaote derivatives were prepared by condensing 2-mercaptobenzothiazole with substituted acid Size: KB.

From Book News, Inc. A class of antitumor agents is discussed in 16 papers, which include explorations of the synthesis, chemical properties, biotransformation, and pharmacokinetics in animals and humans, and studies of analogous agents and substances affecting the mechanism of triazenes. 3-Amino-1,2,4-benzotriazine 1,4-dioxide: Hypoxia-activated antineoplastic agent. A Aminopterin: Folic acid antagonist; blocks thymidine biosynthesis by inhibiting dihydrofolate reductase. More potent, but more toxic, than methotrexate. A Cytosine β-D-arabinofuranoside: Selective inhibitor of DNA synthesis. C C 5-Fluoro


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Synthesis of "bioreversible" derivatives of the anti-tumour agent 2(superior)1-deoxy-5-fluorouridine by Roger Neil Hunston Download PDF EPUB FB2

A practical synthesis of the anti-tumour agent 2-methyldeoxyisopicropodophyllotoxin and related podophyllin analoguesCited by: 7. Design, synthesis, and biological evaluation of novel substituted thiourea derivatives as potential anticancer agents for NSCLC by blocking K-Ras protein-effectors interactions Yuan Zhang, Xin Meng, Haikang Tang, Minghui Cheng, Fujun Yang, and Wenqing XuAuthor: Yuan Zhang, Xin Meng, Haikang Tang, Minghui Cheng, Fujun Yang, Wenqing Xu.

Cancer. 2-Methoxyestradiol (2-MeOE2) 1, an endogenous estrogen metabolite, has emerged as a promising therapeutic candidate for the treatment of a number of conditions. The discovery that 2-MeOE2 inhibits angiogenesis, is anti-proliferative and has in vivo anti-tumour activity 1 has led to its evaluation in phase I/II clinical trials against a range of cancers under the trade name Panzem™.Cited by: Competition assays indicated that bile acids played an important role to carry the derivatives into the bile acid-positive cancer cells.

The results suggest that the introduction of bile acids in the 20th position of camptothecin promote the anti-tumour targeting activity of these derivatives to liver cancer cells. Competition assays indicated that bile acids played an important role to carry the derivatives into the bile acid-positive cancer cells.

The results suggest that the introduction of bile acids in the 20th position of camptothecin promote the anti-tumour targeting activity of these derivatives to liver cancer by: 6. Twenty-nine novel indole-chalcone derivatives were synthesized and evaluated for antiproliferative activity.

Among them, 14k exhibited most potent activity, with IC50 values of 3–9 nM against six cancer cells, which displayed a –fold increase in activity when compare with compound 2.

Further investigation revealed 14k was a novel tubulin polymerization inhibitor binding to the Cited by: derivatives containing various amino groups at position 2, 4 or 6 have been known as anticancer drugs (Sączewski et al., ).

Aiming at discovering new antitumor agents, two different novel series of 1,3,5-triazine derivatives were designed, synthesized and evaluated as potential cytotoxic agents against non-small cell lung cancer (A).Cited by: 4.

Two series of amino acid derivatives containing chrysin were prepared from 7-O-carboxymethyl chrysin (4a) and 7-O-carboxypropyl chrysin (4b) and amino acid methyl esters by treatment with 1-ethyl(3-dimethylaminopropyl)carbodiimide hydrochloride and N-hydroxybenzotriazole as coupling reagents.

The anti-proliferative activities of these derivatives in vitro against human Cited by:   Water-soluble phosphate prodrugs of buparvaquone (1), containing a hydroxynaphthoquinone structure, were synthesized and evaluated in vitro for improved topical and oral drug delivery against cutaneous and visceral leishmaniasis.

The successfull prodrug synthesis involved a strong base; e.g., sodium hydride. Buparvaquonephosphate (4a) and 3-phosphonooxymethyl Cited by: focusing specifically on derivatives bearing cyclic and chiral alkylammonium groups. A library of ten cyclic derivatives and six chiral derivatives were synthesized and fully characterized.

These derivatives have undergone in vitro testing as anti-tumour agents using human lung, ovarian, and cervical carcinoma.

The synthesis of 6-epi-COTC, a diastereoisomer of Streptomyces metabolite 2-crotonyloxymethyl-(4R,5R,6R)-4,5,6-trihydroxycyclohexenone (COTC), is described. The anti-cancer activities of the novel analogue, in racemic and enantiomerically pure forms, are by: Metallated dihydropyran 9 and the dihydropyranone 10 previously used in a synthesis of the insect toxin pederin were adapted to the synthesis of O-methyl mycalamide B, the most potent derivative of the anti-tumour agents isolated from a steps in the synthesis include the oxidation of enol silane 11 from the more hindered face using dimethyldioxirane to introduce the hydroxy group Cited by: Mala Nath, Hitendra Singh, George Eng and Xueqing Song, Synthesis, Structure–Activity Relationship of Some New Triorganotin(IV) Derivatives of Dipeptides as Anti-Inflammatory Agents, Phosphorus, Sulfur, and Silicon and the Related Elements,6, (), ().Cited by:   To prepare the anticancer indoles, a series of substituted heteroannulated indole derivatives has been synthesized and characterized by spectral and elemental analysis.

Subsequently they were evaluated for anticancer activity against cervical cancer (HeLa) cell line using MTT assay. Compounds 5c and 5d exhibit excellent activity with the IC50 value of and µM, Cited by: 5. for guaifenesin maleate prodrug, x guaifenesin succinate prodrug, and x guaifenesin glutarate prodrug.

Half- li v es values (t 1/2) were hours for guaifenesin. The values ofK 1 andK 2 determined by the treatment are in the same relative order as the hydrophobicities of the pyridine homologues:K 1= mM andK 2=54 mM for pyridine.

Marios S. Markoulides and Andrew C. Regan, Synthesis of a phosphinate analogue of the anti-tumour phosphate di-ester perifosine via sequential radical processes, Org.

Biomol. Chem., /C2OBE, 11, 1, (), ().Cited by: A variety of novel bicyclic and tricyclic pyrimidine derivatives was obtained via reaction of 6-aminothioxo-1H-pyrimidineone (1) with a different reagents.

The antimicrobial and anti-inflammatory activities of some of the synthesized compounds were by:   Human tumours are often marked by the expression of unusual carbohydrate structural motifs1–3.

These carbohydrate domains are manifested as cell-surface bound glycolipids or glycoproteins4. This Cited by: 2 C R X R X Fig. 3: Synthesis of 2-benzylbenzimidazole Synthesis of 3-benzoylbenzimidazole derivative: Dissolved gram of the above product in 10 mL of 10% sodium hydrogen carbonate solution and added 1 gram of benzoyl chloride.

The The stopper was removed from time to time since carbon dioxide Compounds R X Y Melting point(°C) Yield (%). Synthesis and in vitro anti-breast cancer activity of some novel 1,5-benzothiazepine derivatives K. L. AMETA*, NITU S. RATHORE and BIRESH KUMAR Department of Chemistry, FASC, Mody Institute of Technology and Science, Deemed University, Lakshmangarh, Rajasthan, India (Received 15 July, revised 19 December ).A very potent anti tumour agent BREAK OR MAKE NEW BONDS.

E J Corey et al BETWEEN ATOMS,Here we not just have many functional groups but. This lecture course is all about doing that kind of. also STEREOCHEMISTRY to think about, The reaction steps are the actual synthesis when When we carry out a reaction one can thus produce. we form.They are also widely used as additives to food and cosmetics and optical brightening agents.

This book deals with the synthesize of new coumarin derivatives by substitution at the third position of hetero-cyclic ring system for novel analgesic and anti-inflammatory agent with minimum toxicity and high : K Arul, Sreeja Sunil.