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Abstract  

This work reports the synthesis, radiolabeling and preliminary biodistribution results in tumor-bearing mice of [99mTc(CO)3(IDA–PEG3–CB)]. The novel chlorambucil derivative was successfully synthesized by conjugation of iminodiacetic acid (IDA) to chlorambucil via a pegylated linker. The ligand could be labeled by [99mTc(CO)3]+ core in high yield to get [99mTc(CO)3(IDA–PEG3–CB)], which was very hydrophilic and was stable at room temperature. Biodistribution studies in tumor-bearing mice showed that [99mTc(CO)3(IDA–PEG3–CB)] accumulated in the tumor with favorable uptake and retention. The good accumulation in tumor tissue with high tumor/muscle ratios warrants further research to improve tumor targeting efficacy and pharmacokinetic profile of radiolabeled chlorambucil derivative by structural modification.

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Abstract  

The search for the lowest energy conformation of complex {β-cyclodextrin (β-CD)+chlorambucil} were carried out by molecular mechanics method. Theoretical calculations of molecular interactions of complex were carried out using the molecular orbital method. The correlation between energy changes and molecular structures are discussed. The large interaction energies calculated by the molecular orbital method bears out the inclusion phenomenon.

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Summary

The evaluation of several derivatization procedures for the gas chromatographic analysis of selected anticancer pharmaceuticals (cyclophosphamide, iphosphamide, flutamide, chlorambucil, and melphalan) in the presence of tricyclic antidepressants was carried out. Among the methods, concerning trimethylsilylation, tert-butyldimethylsilylation, and methylation, the most useful was methylation using (trimethylsilyl)diazomethane (TMSD), which is a safe alternative for the common reaction with diazomethane. Most of the anticancer drugs were unstable during derivatization using silylating agents, while antidepressants were stable in all tested conditions. Melphalan was the only compound, for which the results of all tested procedures were not satisfying. The TMSD-based procedure was validated, giving the results possibly suitable for the screening purposes in contaminated environmental samples.

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Orvosi Hetilap
Authors:
Béla Telek
,
László Rejtő
,
Péter Batár
,
Gyula Reményi
,
Róbert Szász
,
Attila Kiss
, and
Miklós Udvardy

2319 2325 Rai, K. R., Peterson, B. L., Appelbaum, F. R. és mtsai: Fludarabine compared with chlorambucil as primary therapy for chronic lymphocytic leukemia. N

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Orvosi Hetilap
Authors:
Béla Telek
,
György Pfliegler
,
Gyula Reményi
,
Leonóra Méhes
,
Péter Batár
, and
Miklós Udvardy

treatment with fludarbine and chlorambucil: Results of an Intergroup Study, Cancer and Leukemia Group B 9011. J. Clin. Oncol., 2002, 20 , 3878–3884. Peterson B. L. Therapy

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with chlorambucil maintenance chemotherapy. Leuk. Lymphoma, 2006, 47 (11), 2314–2320. 17 Vidal, L., Gurion, R., Ram, R., et al.: Chlorambucil for the

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, B. L.: Impact of therapy with chlorambucil, fludarabine, or fludarabine plus chlorambucil on infections in patients with chronic lymphocytic leukemia: Intergroup Study Cancer and Leukemia

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Oncol. 2016; 17: 928–942. 45 Hillmen P, Gribben JG, Follows GA, et al. Rituximab plus chlorambucil as first-line treatment for chronic lymphocytic leukemia: final analysis of

Open access

Az IGHV mutációanalízis jelentősége krónikus lymphocytás leukémiában

IGHV mutation analysis in chronic lymphocytic leukemia

Hematológia–Transzfuziológia
Authors:
Viktória Fésüs
,
Ediz Eyupoglu
,
Richárd Kiss
,
Emma Ádám
,
András Kozma
,
Zoltán Mátrai
, and
Csaba Bödör

–2282. 22 Goede V, Fischer K, Busch R, et al. Obinutuzumab plus chlorambucil in patients with CLL and coexisting conditions. N Engl J Med. 2014; 370: 1101–1110. 23 Barr

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Orvosi Hetilap
Authors:
Viktória Fésüs
,
Dóra Marosvári
,
Béla Kajtár
,
Péter Attila Király
,
Judit Demeter
,
Tímea Gurbity Pálfi
,
Miklós Egyed
,
Márk Plander
,
Péter Farkas
,
Zoltán Mátrai
,
András Matolcsy
, and
Csaba Bödör

print] 38 Herling, C. D., Klaumünzer, M., Rocha, C. K., et al.: Complex karyotypes, KRAS and POT1 mutations impact outcome in CLL after chlorambucil

Open access