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Nucleic Acids as Therapeutic Targets and Agents
Published in David E. Thurston, Ilona Pysz, Chemistry and Pharmacology of Anticancer Drugs, 2021
Given intravenously, the irritant properties of dacarbazine preclude contact with skin and mucus membranes. Also, because triazenes are prone to photochemical decomposition, an intravenous infusion bag containing dacarbazine must be protected from light. In the UK dacarbazine is used as a single agent to treat metastatic melanoma, and in combination with other agents for soft-tissue sarcomas and Hodgkin’s disease. In particular, it has been used as a component of a combination therapy for Hodgkin’s disease known as ABVD (doxorubicin [AdriamycinTM], Bleomycin, Vinblastine and Dacarbazine). Worldwide, it has also been used in a number of other cancer types including islet cell carcinoma of the pancreas. The predominant side effects are myelosuppression and intense nausea and vomiting.
Halogen Labeled Compounds (F, Br, At, Cl) *
Published in Garimella V. S. Rayudu, Lelio G. Colombetti, Radiotracers for Medical Applications, 2019
Recently, 18F-aryl fluorides of high specific activity were reported by Tewson and Welch128 using a similar reaction. They synthesized piperidyl triazenes as a source of anhydrous diazonium salts. These piperidyl triazenes reacted with 18F-cesium fluoride in the presence of methanesulfonic acid to give organic fluorides of high specific activity. A specific activity of as high as 105 Ci/mmol was achieved. The formation of a reactive intermediate of phenyl cation was proposed as mechanism for the decomposition of the triazene. The reactions were dependent upon the nature of the triazenes and solvents. The radiochemical yields for the fluorination varied from 0.5 to 50%, depending on the substituents on the triazenes.111 Only 0.6 to 7% yield of 18F-spiroperidol was obtained with this approach using bromobenzene as the solvent.128 Similar modification using aryltriazenes with HF-pyridine to prepare aryl fluorides was also presented in a recent meeting.129
Growth of the Ear Capsule
Published in D. Dixon Andrew, A.N. Hoyte David, Ronning Olli, Fundamentals of Craniofacial Growth, 2017
Poswillo (1973) described the pathogenesis of the 1st and 2nd branchial arch syndrome, an asymmetrical dysplasia. The “syndrome includes an array of defects involving not only those derivatives of the first and second arches, and cleft, but also the primordia of the temporal bone. The defects are usually but not invariably unilateral... The most common abnormality is underdevelopment of the external ear, the middle ear ossicles, the condyle and ramus of the mandible, the zygomatic arch and the malar bone. The temporal bone, except for the petrous section housing the internal ear, is frequently involved.” Similar defects were reproduced experimentally in triazene-treated mice of an inbred strain. He suggested that the cause was an embryonic haemorrhage, with the spread of a haematoma explaining the involvement of the temporal bone, not itself a derivative of the branchial arches.
Synthesis and cytotoxic activities of novel copper and silver complexes of 1,3-diaryltriazene-substituted sulfonamides
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2019
Dilek Canakci, Ismail Koyuncu, Nabih Lolak, Mustafa Durgun, Suleyman Akocak, Claudiu T. Supuran
Triazenes (−N = N − NH−) are a diverse group of compounds which have been broadly investigated for synthetic reaction transformations and used for different applications such as natural product synthesis, combinatorial chemistry, and biomedical applications, among others12,13. The 1,3-diaryltriazene scaffold is one of the most interesting core owing to broad biological activities such as antibacteriel, antifungal, efficient carbonic anhydrase inhibitors, and their abundant use is in the development of novel anticancer molecules12,13. On the other hand, triazene compounds of clinical interest (such as Temozolamide and Dacarbazine), are a group of alkylating agents with excellent pharmacokinetic properties and limited toxicity12,13.
Novel sulphonamides incorporating triazene moieties show powerful carbonic anhydrase I and II inhibitory properties
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2020
Sinan Bilginer, Baris Gonder, Halise Inci Gul, Ruya Kaya, Ilhami Gulcin, Baris Anil, Claudiu T. Supuran
Triazenes are an interesting group of compounds which has many applications in the synthesis of various products, some of which possess pharmacological applications16,17. Dacarbazine and temozolomide (Figure 1), both incorporating a triazene moiety, are in the clinical use for cancer treatment, as they possess acceptable toxicity and good pharmacokinetic properties17,18. Additionally, the triazene group is an isostere of the ureido group and was recently reported to lead to interesting CA inhibitory derivatives by Akocak et al.19.
Discovery of novel 1,3-diaryltriazene sulfonamides as carbonic anhydrase I, II, VII, and IX inhibitors
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2018
Suleyman Akocak, Nabih Lolak, Silvia Bua, Claudiu T. Supuran
Triazenes are a diverse group of compounds which are amenable to many synthetic transformations and are also used for different applications, such as natural product synthesis, combinatorial chemistry, and biomedical applications10. On the other hand, triazene compounds of clinical interest (such as Temozolomide and Dacarbazine), are a group of anticancer alkylating agents, with excellent pharmacokinetic properties and limited toxicity10 (Figure 1).