- synthetic pathway- Mechlorethamine, 6-Mercaptopurine
- 6-Mercaptopurine (6-MP)
- IUPAC nomenclature
Methods of Synthesis
In the presence of tetraline as a solvent, hypoxanthine is heated along with excess of phosphorous pentasulfide. These are heated at 200 °C for a few hours
Purine antagonist: 6-Mercaptopurine • These are highly effective antineoplastic drugs. • 6-Mercaptopurine is the thiol analog of hypoxanthine. 6-MP and 6-thioguanine were the first purine analogs to prove beneficial for treating neoplastic disease (Azathioprine, an immunosuppressant, exerts its cytotoxic effects after conversion to 6-MP). • Purine antagonist used for the treatment of malignant diseases (mercaptopurine, thioguanine), but also for immunosuppression (azathioprine) and antiviral chemotherapy (acyclovir, ganciclovir, vidarabine, and zidovudine)
- Nitrogen Mustards Mechlorethamine (Mustine HCl) Cyclophosphamide, Ifosfamide, Chlorambucil, Melphalan 2.Ethylenimine Thio-TEPA 3.Alkyl sulfonate Busulfan 4.Nitrosoureas Carmustine (BCNU), Lomustine (CCNU) 5.Triazine Dacarbazine (OTIC)
- 6. Also knows as Mustine HCl. 1st nitrogen mustard ; highly reactive ; local vesicant . Administration only by IV route . Nausea , vomiting , haemodynamic changes (acute effects) are common side effects. Extravasation during IV injection may cause sloughing. Dose – 0.1 mg/Kg IV daily * 4 days (courses may be repeated at suitable interval).