Melanoma-targeted delivery system (part 2): Synthesis, radioiodination and biological evaluation in B16F0 bearing mice
- Resource Type
- Authors
- Jean-Michel Chezal; Elisabeth Miot-Noirault; Emmanuel Moreau; Radhia El Aissi; Imen Miladi; Olivier Chavignon
- Source
- European Journal of Medicinal Chemistry
European Journal of Medicinal Chemistry, Elsevier, 2016, 120, pp.304-312. ⟨10.1016/j.ejmech.2016.05.019⟩
European Journal of Medicinal Chemistry, Elsevier, 2016, 120, pp.304-312. 〈10.1016/j.ejmech.2016.05.019〉
- Subject
- Drug
Biodistribution
media_common.quotation_subject
[CHIM.THER]Chemical Sciences/Medicinal Chemistry
Pharmacology
010402 general chemistry
01 natural sciences
Iodine Radioisotopes
Mice
03 medical and health sciences
0302 clinical medicine
Pharmacokinetics
[ CHIM.ORGA ] Chemical Sciences/Organic chemistry
Idoxuridine
Drug Discovery
medicine
Animals
Humans
Prodrugs
Tissue Distribution
[CHIM.COOR]Chemical Sciences/Coordination chemistry
Melanoma
ComputingMilieux_MISCELLANEOUS
media_common
Biological evaluation
Chemistry
[CHIM.ORGA]Chemical Sciences/Organic chemistry
Organic Chemistry
[ CHIM.COOR ] Chemical Sciences/Coordination chemistry
[ CHIM.THER ] Chemical Sciences/Medicinal Chemistry
General Medicine
Prodrug
medicine.disease
Xenograft Model Antitumor Assays
0104 chemical sciences
3. Good health
030220 oncology & carcinogenesis
Delivery system
Radiopharmaceuticals
[ CHIM.RADIO ] Chemical Sciences/Radiochemistry
[CHIM.RADIO]Chemical Sciences/Radiochemistry
medicine.drug
- Language
- English
- ISSN
- 0223-5234
1768-3254
Here we report the synthesis and radiolabelling with iodine-125 of a melanoma-selective prodrug (17a*) and its parent drug IUdR. The in vivo and ex vivo biodistributions of [(125)I](17a*) and [(125)I]IUdR were evaluated in a model of melanoma B16F0-bearing mice. The pharmacokinetic profile of [(125)I](17a*) suggests rapid release of the active drug [(125)I]IUdR after i.v. administration of [(125)I](17a*). Preliminary metabolism studies in dedicated compartments (i.e. blood, urine and tumour) yielded results consistent with this hypothesis.