Antineoplastic Agents Flashcards
Alkylating agents used as Antineoplastic
Nitrosoureas (Carmustine, Lomustine, Semustine)
Nitrogen Mustards (Cyclophosphamide, Ifosfamide)
Thiotepa
Busulfan
Mechlorethamine
Chlorambucil
MOA of Nitrosoureas
Form covalent bonds with nucleophilic groups present on DNA – alkylation of DNA leads to cell death
Nitrosoureas undergo spontaneous 1. _______ ______ with the formation of the 2. _______ ______ ____ from diazohydroxide formed.
- non-enzymatic degradation
2. 2-chloroethyl carbonium ion
Nitrosoureas activates DNA by liberating isocyanate that attach carboxyl groups to the lysine residues of proteins.
True or False
False!!
Nitrosoureas INACTIVATES DNA by liberating isocyanate that attach CARBAMOYL groups to the lysine residues of proteins.
An alkylating agent that is used for the treatments of Hodgkin’s Lymphoma and Chronic lymphocytic leukemia (CLL) with prednisone.
Chlorambucil
Utilizes two sulfonate functionalities as leaving grps separated by a four-carbon chain that reacts with DNA.
Busulfan
MOPP treatment of Hodgkin’s Lymphoma
Mechlorethamine, Oncovin (vincristine), procarbazine, and prednisone
A member of aziridines that is an active alkylating agent.
Thiotepa
Platinum-Based Antineoplastic Agents
Cisplatin, Oxaliplatin, Carboplatin
Antineoplastic Agents that are structurally related to natural metabolite necessary for cellular growth, Inhibit the production of utilization of these metabolites.
Antimetabolites
Drugs under Purine Analogs (M,T,A,P)
Mercaptopurine, Thioguanine, Azathioprine, Pentostatine
Pyrimidine Analogs (F,F,C,G)
Fluorouracil, Fluxuridine, Cytarabine, Gemcitabine
Folic Acid Analog
Methotrexate
These antibiotics disrupt DNA function and cell division.
Cytotoxic Antibiotics
MOA of Cytotoxic Antibiotics
Planar molecule inserts itself between base pair of DNA (-) topoisomerase