2016
DOI: 10.1002/jlcr.3481
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Synthesis and preliminary biological evaluation of a99mTc-chlorambucil derivative as a potential tumor imaging agent

Abstract: Technetium-99m-based radiopharmaceuticals have been used widely as diagnostic agents in the nuclear medicine. Chlorambucil (CLB) as one typical alkylating drug exhibits excellent inhibition effects against many human malignancies. To develop and explore a novel potential imaging agent for early diagnosis of tumors, tricarbonyl technetium-99m and rhenium complexes on the basis of the tridentate ligand dipicolylamine (DPA) bound to the chlorambucil pharmacophore were designed and synthesized: Tc-DPA-CLB (3) and … Show more

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Cited by 12 publications
(8 citation statements)
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“…The chemotherapeutic drug CLB radiolabeled with 99m Tc-tricarbonyl core using 2 different chelators containing N 2 O and NNN as donor atoms has been reported. 25,26 The 2 99m Tc(CO) 3 -labeled CLB complexes had high log P values of 1.2 and 2.34, respectively, and thus exhibited high liver and intestinal activities. 99m Tc(CO) 3 -CLB complex with N 2 O donors showed increase in the stomach activity indicating decomposition of the radiotracer.…”
Section: Biodistribution Studiesmentioning
confidence: 99%
“…The chemotherapeutic drug CLB radiolabeled with 99m Tc-tricarbonyl core using 2 different chelators containing N 2 O and NNN as donor atoms has been reported. 25,26 The 2 99m Tc(CO) 3 -labeled CLB complexes had high log P values of 1.2 and 2.34, respectively, and thus exhibited high liver and intestinal activities. 99m Tc(CO) 3 -CLB complex with N 2 O donors showed increase in the stomach activity indicating decomposition of the radiotracer.…”
Section: Biodistribution Studiesmentioning
confidence: 99%
“…It exhibits high initial tumor uptake with certain retention, fast clearance from background, good tumor/background ratios, and satisfactory scintigraphic images; all of which highlight the potential of 99m Tc(CO) 3 (His‐CB) as a tumor imaging agent . Lin et al have reported the latest research on a new 99m Tc(CO) 3 ‐labeled chlorambucil analog DPA‐CLB, which has the property of favorable tumor uptake and retention, fast clearance from background, and good T/NT ratios, suggesting that it has potential as a tumor imaging agent for breast cancer …”
Section: Introductionmentioning
confidence: 99%
“…6 Lin et al have reported the latest research on a new 99m Tc(CO) 3 -labeled chlorambucil analog DPA-CLB, which has the property of favorable tumor uptake and retention, fast clearance from background, and good T/NT ratios, suggesting that it has potential as a tumor imaging agent for breast cancer. 7 Melphalan has been labeled with 125 I directly to get [ 125 I]Melphalan, which has a high affinity to be localized in the tumor site and meets most of the requirements necessary to be used as a successful diagnostic and therapeutic agent. 8 We have synthesized a novel MFL derivative by conjugation of HYNIC to MFL, which is labeled by 99m Tc in high yield to get 99m Tc(HYNIC-MFL)(tricine)(TPPTS).…”
Section: Introductionmentioning
confidence: 99%
“…Chlorambucil (CLB), a commercially available nitrogen mustard drug, has been widely used against a variety of cancers including chronic lymphocytic leukemia, ovarian cancer, breast cancer, lymphomas, and some other malignancies. Chlorambucil produces its cytotoxic effects by the two reactive chloroethyl side chains which bind preferably to the N7 atoms of guanine bases, causing interstrand and intrastrand linking of DNA, , and thus leading to halted DNA replication and DNA damage. However, chlorambucil has low solubility and easily suffers from rapid degradation in an aqueous environment, resulting in a short half-life in vivo .…”
Section: Introductionmentioning
confidence: 99%