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Relevant bibliographies by topics / Antimetabolite drugs

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Academic literature on the topic 'Antimetabolite drugs'

Author: Grafiati

Published: 5 June 2025

Last updated: 24 June 2025

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Journal articles on the topic "Antimetabolite drugs"

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Shewach, Donna S., and Theodore S. Lawrence. "Antimetabolite Radiosensitizers." Journal of Clinical Oncology 25, no. 26 (2007): 4043–50. http://dx.doi.org/10.1200/jco.2007.11.5287.

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Radiosensitization with antimetabolites has improved clinical outcome for patients with solid malignancies, especially cancers of the GI tract, cervix, and head and neck. Fluorouracil (FU) and hydroxyurea have been widely used clinically during the last four decades, and promising results have been observed more recently with gemcitabine. Although the antimetabolites all target DNA replication, they differ with respect to the mechanisms by which they produce radiosensitization. The antimetabolite radiosensitizers may inhibit thymidylate synthase (TS) or ribonucleotide reductase, and the nucleoside/nucleobase analogs can be incorporated into DNA. Radiosensitization can result from chemotherapy-induced increase in DNA double-strand breaks or inhibition of their repair. Studies of repair pathways involved in radiosensitization with antimetabolites implicate base excision repair with the TS inhibitors, homologous recombination with gemcitabine, and mismatch repair with FU and gemcitabine. Gemcitabine can also stimulate epidermal growth factor receptor (EGFR) phosphorylation; inhibiting this effect with EGFR inhibitors can potentiate cytotoxicity and radiosensitization. Additional work is necessary to determine more precisely the processes by which antimetabolites act as radiation sensitizers and to define the optimal sequencing of these agents with EGFR inhibitors to provide better guidance for clinical protocols combining these drugs with radiotherapy.

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Poonam, Jaiswal, K. Dwivedi P., and C. Shukla I. "Assay of some biologically active antimetabolite antineoplastic drugs with N-bromosuccinimide reagent." Journal of Indian Chemical Society Vol. 82, Nov 2005 (2005): 1027–29. https://doi.org/10.5281/zenodo.5825128.

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Department of Chemistry, University of Allahabad, Allahabad-211 002, India <em>E-mail</em>: poonamjai92@rediffmail.com  Poonam_J9672000@yahoo.com <em>Manuscript received 8 October 2004, revised 10 August 2005. accepted 17 August 2005</em> In the present investigation a simple, sensitive, selective, quick and convenient method has been developed for the determination of some antimetabolite drugs e.g. methotrexate, mercaptopurine and 5-tluorouracil in pure form and in their pharmaceutical preparations.

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Chatterjee, Manosree, Ritwik Maity, Souvik Das, Nibedita Mahata, Biswarup Basu, and Nripen Chanda. "Electrospray-based synthesis of fluorescent poly(d,l-lactide-co-glycolide) nanoparticles for the efficient delivery of an anticancer drug and self-monitoring its effect in drug-resistant breast cancer cells." Materials Advances 1, no. 8 (2020): 3033–48. http://dx.doi.org/10.1039/d0ma00646g.

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A novel approach used to synthesize antimetabolite-conjugated and intense blue fluorescence-emitting smart polymeric nanoparticles is reported for the efficient delivery of anticancer drugs and self-monitoring their effect in drug-resistant metastatic breast cancer cells.

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Bolletta, Elena, Marco Coassin, Danilo Iannetta, et al. "Cataract Surgery with Intraocular Lens Implantation in Juvenile Idiopathic Arthritis-Associated Uveitis: Outcomes in the Era of Biological Therapy." Journal of Clinical Medicine 10, no. 11 (2021): 2437. http://dx.doi.org/10.3390/jcm10112437.

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This study compared the outcomes of cataract surgery with intraocular lens (IOL) implantation in patients with juvenile idiopathic arthritis (JIA)-associated chronic anterior uveitis treated with antimetabolite drugs and systemic corticosteroids (Non-Biological Group) versus patients treated with antimetabolites and biological drugs (Biological Group). A cohort of patients with cataract in JIA-associated uveitis undergoing phacoemulsification with IOL implantation was retrospectively evaluated. The main outcome was a change in corrected distance visual acuity (CDVA) in the two groups. Ocular and systemic complications were also recorded. The data were collected preoperatively and at 1, 12, and 48 months after surgery. Thirty-two eyes of 24 children were included: 10 eyes in the Non-Biological Group and 22 eyes in the Biological Group. The mean CDVA improved from 1.19 ± 0.72 logMAR preoperatively to 0.98 ± 0.97 logMAR at 48 months (p = 0.45) in the Non-Biological Group and from 1.55 ± 0.91 logMAR preoperatively to 0.57 ± 0.83 logMAR at 48 months (p = 0.001) in the Biological Group. The postoperative complications, including synechiae, cyclitic membrane, IOL explantation, glaucoma, and macular edema, were not statistically different between the two groups. An immunosuppressive treatment with biological drugs can improve the visual outcome after cataract surgery in patients with JIA-associated uveitis, but it does not significantly reduce postoperative ocular complications.

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Galor, Anat, Douglas A. Jabs, Henry A. Leder, et al. "Comparison of Antimetabolite Drugs as Corticosteroid-Sparing Therapy for Noninfectious Ocular Inflammation." Ophthalmology 115, no. 10 (2008): 1826–32. http://dx.doi.org/10.1016/j.ophtha.2008.04.026.

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Hammersmith, K. M. "Comparison of Antimetabolite Drugs as Corticosteroid-Sparing Therapy for Noninfectious Ocular Inflammation." Yearbook of Ophthalmology 2009 (January 2009): 100–103. http://dx.doi.org/10.1016/s0084-392x(09)79166-x.

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Buchanich, Jeanine M., Craig W. Newcomb, Terri L. Washington, et al. "Use of immunosuppression and subsequent cancer incidence: cohort study." BMJ Oncology 2, no. 1 (2023): e000037. http://dx.doi.org/10.1136/bmjonc-2023-000037.

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ObjectiveEvaluate the association between cancer incidence and immunosuppressive treatment in patients with ocular inflammatory disease (OID).Methods and analysisWe performed a retrospective cohort study of patients from 10 US OID subspecialty practices. Patients with non-infectious OID were included; HIV-infected patients were excluded. Time-dependent exposure to drug classes (ie, antimetabolites, calcineurin inhibitors, alkylating agents, tumour necrosis factor (TNF) inhibitors) and drugs were evaluated. Cancer incidence was ascertained by linkage to 12 state cancer registries from 1996 to 2015. Cancer incidence was analysed using Cox regression survival analysis, using 0-year, 3-year and 5-year lags after immunosuppression began.ResultsThe cancer incidence cohort comprised 10 872 individuals at risk of incident cancer and residing in one of the 12 states covered; 812 primary cancers were identified through cancer incidence tracing with median follow-up time of 10 years. Neither TNF inhibitor, antimetabolite, calcineurin inhibitor nor alkylating agent classes were associated with statistically significant increases in cancer incidence adjusting for covariates. We found statistically significant reduced hazards in the systemic inflammatory disease (SID)-including cohort for adalimumab and chlorambucil, increased hazards for tacrolimus and etanercept in the non-SID cohort and reduced hazards for methotrexate in both. Other immunosuppressive drugs were not associated with overall cancer incidence.ConclusionsWe found no increased risk of overall or site-specific cancer incidence associated with short-term (non-transplant) therapy with most commonly used immunosuppressive drug classes and many specific drugs. Further research may clarify potentially protective or harmful effects of specific agents that were not consistently associated with reduced or increased cancer incidence.Trial registration numberNCT00116090.

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Perello, Laurent, Sylvie Demirdjian, Alexandre Dory, and Philippe Bourget. "Application of High-Performance, Thin-Layer Chromatography to Quality Control of Antimetabolite Analogue Infusion Bags." Journal of AOAC INTERNATIONAL 84, no. 4 (2001): 1296–300. http://dx.doi.org/10.1093/jaoac/84.4.1296.

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Abstract A global postproduction quality program was developed to secure chemotherapy infusion at the Gustave Roussy Institute. Despite rigorous procedures and computerized prescriptions, an analytical check was necessary to improve the quality of ready-to-use solutions of cytotoxic drugs in our Centralized Antineoplastics Reconstitution Unit. High-performance, thin-layer chromatography was selected as the analytical tool to assay 12 anticancer drugs. One of the analytical methods can separate 4 antimetabolite substances, i.e., fludarabine (FDB), cytarabine (CTB), gemcitabine (GTB), and fluorouracil (5 FU). For all infusion bags manufactured, up to 26 samples could be assayed per series using a double standard calibration (GTB and 5 FU).

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Castellví, Marc, Eudald Felip, Ifeanyi Ezeonwumelu, et al. "Pharmacological Modulation of SAMHD1 Activity by CDK4/6 Inhibitors Improves Anticancer Therapy." Cancers 12, no. 3 (2020): 713. http://dx.doi.org/10.3390/cancers12030713.

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Sterile alpha motif and histidine-aspartic acid domain-containing protein 1 (SAMHD1) is a dNTP triphosphohydrolase involved in the regulation of the intracellular dNTP pool, linked to viral restriction, cancer development and autoimmune disorders. SAMHD1 function is regulated by phosphorylation through a mechanism controlled by cyclin-dependent kinases and tightly linked to cell cycle progression. Recently, SAMHD1 has been shown to decrease the efficacy of nucleotide analogs used as chemotherapeutic drugs. Here, we demonstrate that SAMHD1 can enhance or decrease the efficacy of various classes of anticancer drug, including nucleotide analogues, but also anti-folate drugs and CDK inhibitors. Importantly, we show that selective CDK4/6 inhibitors are pharmacological activators of SAMHD1 that act by inhibiting its inactivation by phosphorylation. Combinations of a CDK4/6 inhibitor with nucleoside or folate antimetabolites potently enhanced drug efficacy, resulting in highly synergic drug combinations (CI < 0.04). Mechanistic analyses reveal that cell cycle-controlled modulation of SAMHD1 function is the central process explaining changes in anticancer drug efficacy, therefore providing functional proof of the potential of CDK4/6 inhibitors as a new class of adjuvants to boost chemotherapeutic regimens. The evaluation of SAMHD1 expression in cancer tissues allowed for the identification of cancer types that would benefit from the pharmacological modulation of SAMHD1 function. In conclusion, these results indicate that the modulation of SAMHD1 function may represent a promising strategy for the improvement of current antimetabolite-based treatments.

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Singh, Rohit K., Ajit Kishor, Dev R. Rishu, Rashmi Asha, Keshav K. Sinha, and Rani I. Sinha. "Immunosuppressive drugs in renal transplantation." International Journal of Basic & Clinical Pharmacology 12, no. 2 (2023): 303–12. http://dx.doi.org/10.18203/2319-2003.ijbcp20230405.

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A kidney transplant, sometimes known as a renal transplant, is the treatment of choice for kidney failure at end stage renal disease (ESRD). The renal transplant surgery is followed by a lifetime course of immunosuppressive agents, divided into initial induction phase and later maintenance phase. It is seen that the risk of acute rejection is maximum in the initial months after transplantation (induction phase) and then reduces later (maintenance phase). In induction phase there is use of high-intensity immunosuppression immediately after transplantation, when the risk of rejection is maximum and then the dose reduced for long- term therapy. The main challenge in the renal transplantation community is long- term transplant survival. Long-term graft loss is mainly due to acute and chronic graft rejection, and also due to complications of immunosuppressive therapy. Currently, there is triple therapy as conventional immunosuppressive protocol: a calcineurin inhibitor, an antimetabolite agent, and a corticosteroid. The main aim of development of new immunosuppressive agents is not only improvement of short- term outcomes but also to increase the long- term graft survival by less nephrotoxicity, and minimal side-effects.

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Dissertations / Theses on the topic "Antimetabolite drugs"

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Samuels, C. S. "An evaluation of 6-thioguanine derivatives as potential anti-cancer agents." Pretoria : [s.n.], 2008. http://upetd.up.ac.za/thesis/available/etd-11262009-174642/.

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Tiwari, Rohit. "COMPUTATIONAL AND SYNTHETIC STUDIES ON ANTIMETABOLITES FOR ANTICANCER-, ANTIVIRAL-,AND ANTIBIOTIC DRUG DISCOVERY." The Ohio State University, 2010. http://rave.ohiolink.edu/etdc/view?acc_num=osu1267819591.

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Fotoohi, Alan Kambiz. "Pharmacological and molecular investigations on the mechanisms underlying resistance of human leukaemia cells to the antimetabolites methotrexate, 6-mercaptopurine and 6-thioguanine /." Stockholm, 2007. http://diss.kib.ki.se/2007/978-91-7357-087-9/.

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Serviant-Fine, Thibaut. "Une approche rationnelle de la chimiothérapie : histoire des antimétabolites (1935-1955)." Thesis, Lyon, 2016. http://www.theses.fr/2016LYSE1271/document.

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En 1940, le biochimiste anglais Donald Woods propose une explication du mode d'action des nouveaux sulfamides antibactériens : l'inhibition compétitive. Son collègue Paul Fildes fonde sur cette base une nouvelle approche de la chimiothérapie, revendiquée comme rationnelle, un programme pour la recherche de nouveaux médicaments. Cette thèse explore l'impact de la théorie des antimétabolites, comme elle sera appelée, dans la recherche biochimique et pharmaceutique. La première partie retrace son élaboration dans le contexte de l'école de biochimie anglaise, puis sa reprise aux États-Unis à la suite de travaux menés en parallèle sur les vitamines. La seconde partie est consacrée au développement de deux programmes de recherche distincts dédiés aux antimétabolites, illustrant les modalités et fortunes divergentes d'appropriation de cette approche rationnelle. Le premier est une collaboration modeste entre le biochimiste Henry McIlwain et la firme pharmaceutique Glaxo pendant la guerre au Royaume-Uni. Le second consiste en la mise en place du programme de George Hitchings et Gertrude Elion chez Burroughs Wellcome aux États-Unis, souvent considéré comme l'origine du rational drug design actuel. La théorie des antimétabolites correspond aussi bien à l'ambition d'obtenir des chimiothérapies spécifiques qu'à un ensemble de pratiques dans le quotidien du laboratoire<br>In 1940, the British biochemist Donald Woods put forward an explanation of the mode of action of the new antibacterial sulfa drugs, competitive inhibition. His colleague, Paul Fildes, developed this work into a new approach to chemotherapy, which he qualified as a rational programme for drug discovery. This dissertation explores the impact of the theory of antimetabolites, as it came to be known, in biochemical and pharmaceutical research. The first part traces its development in the context of the British school of biochemistry and its further expansion in the United States following parallel research on vitamins. The second part deals with the construction of two distinct research programmes dedicated to antimetabolites, each one illustrating a different way of following this rational approach and their varying consequences. The first one is a modest collaboration between the biochemist Henry McIlwain and the Glaxo pharmaceutical company during the war in the United Kingdom. The second one corresponds to the establishment of George Hitchings' and Gertrude Elion's programme at Burroughs Wellcome in the United States, often considered as the origin of today's rational drug design. The theory of antimetabolites simultaneously embodied both the ambition of attaining specific chemotherapies, and a set of practices in day-to-day laboratory work

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Matsutani, Guilherme Costa. "Antimaláricos potenciais: planejamento e síntese de fármacos dirigidos de antimetabólitos de serina." Universidade de São Paulo, 2008. http://www.teses.usp.br/teses/disponiveis/9/9138/tde-27102016-104221/.

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De acordo com a Organização Mundial da Saúde, AIDS,malária e tuberculose são as três maiores doenças infectantes do mundo, atingindo principalmente crianças. Regiões paupérrimas e de clima tropical, como a África sub-saariana, são as mais atingidas. Este quadro agrava-se com a disseminação de cepas do Plasmodium falciparum resistentes à cloroquina e multi-resistentes.Além disso, alguns fármacos utilizados na terapêutica da malária apresentam vários efeitos adversos, comprometendo o tratamento. Trata-se de um grande desafio e o seu enfrentamento requer estratégias. O desenvolvimento de novos quimioterápicos deve fundamentar-se em diferenças bioquímicas e morfológicas entre as células do hospedeiro e do parasita. A biossíntese de fosfolipídeos de membrana em parasitas do grupo Apicomplexa é de extrema importância para a maturação e a reprodução do parasita e constitui-se em bom alvo para novos antimaláricos, uma vez que é encontrada somente em parasitas. Hemácias infectadas têm sua absorção modificada em relação aos eritrócitos não-infectados, conferindo seletividade a substâncias como lipídeos. O trabalho em questão propõe a síntese de antimetabólitos da serina, visando à inibição das enzimas fosfatidilserina síntase e serina descarboxilase, fundamentais para a biossíntese de fosfolipídeos de membrana desses parasitas.. Cinco derivados heterocíclicos da serine foram sintetizados: derivados diidroimidazólico, diidroxazólico, diidroxazínico, diidropirimidínico e diidrooxatiólico. Também, o transportador fosfolipídico com o ácido esteárico foi sintetizado. Os antimetabólitos serão acoplados a esse e outros fosfolipídeos, obtendo-se fármacos dirigidos específicos direcionados seletivamente a eritrócitos infectados.<br>According to the World Health Organization, Aids, malaria and tuberculosis are the three greatest infectious diseases in the world. Children are the most involved in those diseases. Extremely poor regions, as sub-Saharan, Africa, are the most affected. In the worst case scenario, one of the parasites that causes malaria, Plasmodium falciparum, become resistant to chloroquine and the current therapy. Besides, some drugs used in the mataria chemotherapy are very toxic, showing many side effects, and compromising the treatment. This is a big challenge and facing it requires new strategies.. The development of chemotherapeutic has been inspired in biochemical differences between the parasite and the host. Plasmodíum falciparum needs to biosynthesize phospholipids for their membrane. These phospholipids are very important to the maturation and reproduction of the parasite and occur only in it.. This makes the phospholipids biosynthesis a good target for new and specific antimalarial drug design. Infected red blood cell shows modified permeation, allowing the lipids to be freely transported, what is not usual in the non-infected red blood cells. This said, in the present work the design and synthesis of serine metabolic inhibitors, using the bioisosteric strategy, have been proposed. The inhibition of the phosphatidylserine biosynthesis, an important phospholipid, is expected. These inhibitors will be linked to phospholipids, to promote the selective permeation to the infected red-blood cell.. These inhibitors will be linked to phospholipids, to promote the selective permeation to the infected redblood cell. In the present work five heterocyclic serine inhibitors: diidroimidazolic, diidroxazolic, diidroxazinico, diidropyriminic and diidroxatiolic. Also synthesized a phospholipid to be connected to the heterocyclic inhibitors.

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Månsson, Emma. "Resistance mechanisms for nucleoside analogues - with focus on metabolism and apoptosis /." Stockholm : [Karolinska institutets bibl.], 2002. http://diss.kib.ki.se/2002/91-7349-330-9/.

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Books on the topic "Antimetabolite drugs"

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S, Gupta Radhey, ed. Drug resistance in mammalian cells. CRC Press, 1989.

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M, Rustum Youcef, ed. Fluoropyrimidines in cancer therapy. Humana Press, 2003.

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Anticancer drugs: Antimetabolite metabolism and natural anticancer agents. Pergamon Press, 1994.

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Powis, Garth. Anticancer Drugs: Antimetabolite Metabolism and Natural Anticancer Agents. Elsevier Science Pub Co, 1994.

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Powis, Garth. Anticancer Drugs: Antimetabolite Metabolism and Natural Anticancer Agents. Elsevier Science Pub Co, 1994.

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Matti S., M.D. Aapro. Innovative Antimetabolites in Solid Tumours (Eso Monographs (European School of Oncology)). Springer-Verlag Telos, 1994.

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Gupta, Radhey S. Drug Resistance in Mammalian Cells: Antimetabolite and Cytotoxic Analogs. Crc Pr I Llc, 1989.

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Antifolate drugs in cancer therapy. Humana Press, 1999.

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Kulkarni, Kunal, James Harrison, Mohamed Baguneid, and Bernard Prendergast, eds. Renal medicine. Oxford University Press, 2016. http://dx.doi.org/10.1093/med/9780198729426.003.0016.

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Nephrology is a relatively young specialty, which has seen several outstanding achievements in medicine such as the success of dialysis and transplantation. Empirical developments, such as the treatment of renal disease with drugs such as corticosteroids and antimetabolites, have also been successful. However, there is little evidence regarding the best way to apply these treatments. Doing randomized trials of effective treatments is tricky, especially as many nephrologists are confident they have identified the right way to do things. Slowly, this mindset is being changed; prejudices are being challenged, and old, as well as new, treatments properly tested. This section describes some of the investigations that have persuaded some clinicians to make changes to their clinical practice.

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Rustum, Youcef M. Fluoropyrimidines in Cancer Therapy. Humana Press, 2010.

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Book chapters on the topic "Antimetabolite drugs"

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Thurston, David E., and Ilona Pysz. "Antimetabolites." In Chemistry and Pharmacology of Anticancer Drugs, 2nd ed. CRC Press, 2021. http://dx.doi.org/10.1201/9781315374727-3.

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Kim, Kyu-Won, Jae Kyung Roh, Hee-Jun Wee, and Chan Kim. "Antimetabolic Anticancer Drugs." In Cancer Drug Discovery. Springer Netherlands, 2016. http://dx.doi.org/10.1007/978-94-024-0844-7_5.

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Bhattacharjee, Mrinal K. "Antimetabolites: Antibiotics That Inhibit Nucleotide Synthesis." In Chemistry of Antibiotics and Related Drugs. Springer International Publishing, 2016. http://dx.doi.org/10.1007/978-3-319-40746-3_4.

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Bhattacharjee, Mrinal K. "Antimetabolites: Antibiotics That Inhibit Nucleotide Synthesis." In Chemistry of Antibiotics and Related Drugs. Springer International Publishing, 2022. http://dx.doi.org/10.1007/978-3-031-07582-7_4.

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O’Dwyer, Peter J. "Biochemical modulation as an approach to reversal of antimetabolite resistance." In Anticancer Drug Resistance. Springer US, 1994. http://dx.doi.org/10.1007/978-1-4615-2632-2_10.

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Moran, Richard G. "Folate antimetabolites inhibitory to de novo purine synthesis." In New Drugs, Concepts and Results in Cancer Chemotherapy. Springer US, 1992. http://dx.doi.org/10.1007/978-1-4615-3876-9_4.

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Herschler, J., J. S. Kay, B. S. Litin, and M. Chvapil. "Drug Delivery of Antimetabolites as Adjuncts to Glaucoma Filtration Surgery: Preliminary Clinical Experience." In Glaucoma Update III. Springer Berlin Heidelberg, 1987. http://dx.doi.org/10.1007/978-3-642-71785-7_31.

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Duncan, Richards, and Jeffrey Aronson. "Drugs used to treat cancer: Antimetabolite drugs: BNF 8.1.3, 10.1.3, and 13.5.2." In Oxford Handbook of Practical Drug Therapy. Oxford University Press, 2005. http://dx.doi.org/10.1093/med/1.1.med-9780198530077-div1-164.

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"Antimetabolites." In Antineoplastic Drugs. John Wiley & Sons, Ltd, 2015. http://dx.doi.org/10.1002/9781118892572.ch2.

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Avendaño, Carmen, and J. Carlos Menéndez. "Antimetabolites." In Medicinal Chemistry of Anticancer Drugs. Elsevier, 2008. http://dx.doi.org/10.1016/b978-0-444-52824-7.00002-0.

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Conference papers on the topic "Antimetabolite drugs"

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Merenkova, Ievgeniia, Yaroslav Dziublyk, and Galyna Gumeniuk. "Comparative analysis of the efficacy of glucocorticosteroids and antimetabolite drugs in treatment of patients with pulmonary sarcoidosis." In ERS International Congress 2019 abstracts. European Respiratory Society, 2019. http://dx.doi.org/10.1183/13993003.congress-2019.pa1945.

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Arnautova, A. O., I. A. Aleksakhina, A. L. Kayushin, and I. D. Konstantinova. "NEW BENZIMIDAZOLE NUCLEOSIDES." In OpenBio-2023. ИПЦ НГУ, 2023. http://dx.doi.org/10.25205/978-5-4437-1526-1-46.

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Modified nucleosides are one of the most important classes of antimetabolites actively used in practical medicine as antiviral and antitumor drugs. There are two main methods of producing nucleoside analogs: chemical and enzymatic. The purpose of this study is to develop an efficient method for the preparation of new benzimidazole nucleosides by enzymatic synthesis.

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Birichevskaya, L. L., M. A. Vinter, A. A. Doroshevich, M. А. Khancheuski, E. I. Kvasyuk, and A. I. Zinchenko. "SYNTHESIS OF THE MODIFIED NUCLEOSIDE 8-BROMADENOSINE AND ITS PHOSPHOLIPID DERIVATIVE." In SAKHAROV READINGS 2021: ENVIRONMENTAL PROBLEMS OF THE XXI CENTURY. International Sakharov Environmental Institute of Belarusian State University, 2021. http://dx.doi.org/10.46646/sakh-2021-2-20-23.

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Modified nucleoside 8-bromoadenosine possessing high reactive capacity may serve as a basic compound for the synthesis of a large number of purine antimetabolites showing potentially therapeutic activities toward several tumor and viral diseases. In this study, 8-bromoadenosine was produced by a simple eco-friendly procedure following the treatment of nucleoside precursor adenosine with aqueous bromine solution. In the course of enzymatic transphosphatidylation reaction, the first synthesis of phospholipid derivative of the above-mentioned nucleoside -5‘-(1,2-dimyristoyl phosphatidyl)-8-bromoadenosine was accomplished. Novel compounds may presumably act as non-toxic progenitors of bioactive antimetabolites to be used in drug formulas.

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Chang, Shih-Shin, Hirohito Yamaguchi, and Mien-Chie Hung. "Abstract B03: Cisplatin-resistant cells possess collateral sensitivity to folate antimetabolites." In Abstracts: AACR Precision Medicine Series: Drug Sensitivity and Resistance: Improving Cancer Therapy; June 18-21, 2014; Orlando, FL. American Association for Cancer Research, 2015. http://dx.doi.org/10.1158/1557-3265.pms14-b03.

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Felip, Eudald, Roger Badia, Mireia Margelí, et al. "Abstract P5-05-14: Cyclin-dependent kinases inhibitors improve antimetabolite drug potency depending on SAMHD1 expression." In Abstracts: 2019 San Antonio Breast Cancer Symposium; December 10-14, 2019; San Antonio, Texas. American Association for Cancer Research, 2020. http://dx.doi.org/10.1158/1538-7445.sabcs19-p5-05-14.

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