Anticancer Flashcards
Quiescence
G0 phase in which cells are not dividing
Mitosis
—Prophase chromosomes appear condensed and nuclear envelope breaks down
—Metaphase microtubules from centrioles align chromosomes in the middle
—Anaphase chromosomes separate and move to opposite sides
—-Telophase & cytokinesis nuclear membrane forms around separated xsomes and cell wall pinch off
After, new cells return to G1 to divide again or go into Go phase
Checkpoints
Surveillance mechanisms to ensure each phase completes properly before next. Some cells can bypass these like cancer
G1
G2
M
Bleomycin
Anti cancer antibiotic works by free oxygen radicals formation
Used for Hodgkin’s lymphoma, squamous cell carcinomas, testicular cancer
SE skin hyperpigmentation, mucositis/stimatitis, pulmonary fibrosis
Dactomycin (actinomycin D)
Anti cancer antibiotic
Topoisomerase inhibitor and free oxygen radical formation
-Used pediatric cancer, erwings sarcoma
SE bone marrow suppression
Anthracyclines
Doxorubicin, daunorubicin
Topoisomerase inhibitor and free radical formation
Lymphoma, solid tumors, thyroid cancer, leukemia
SE bone marrow suppression, dilated cardiomyopathy
Alkylating agents
Adds alkyl group to guanine and is not cell cycle specific
-Cyclophosmamide (are nitrogen mustards prodrug) eg ifosmide, mechlorethamine
-Busulfan
-Nitrosoureas (can cross BBB) so used for brain turmors
-Procarbozine (mechanism unknown)
Nitrosoureas
Carmustine, Lomustine and streptozocin
Require activation by cyp450
Can cross BBB so used for brain tumors like glioblastoma multiforme
SE Convulsions, seizures and ataxia
Cell cycle
- Interphase
Go no growth or resting
G1 grows and does function
S DNA replication
G2 cell grows - Mitosis
PMAT and c
Monofunctional alkylating agents
Alkylate single site
Can cause carcinogenesis(cause DNS repair will be attempted) or cell death
Eg procarbazine, carmustine, dacarbazine, streptozocin, temozolomide
Bifunctional alkylating agents
Cross linking of 2 guanine bases causing cross bridges on DNA
So DNA cannot separate for transcription wc can lead to cell death
Nitrogen mustard
Cyclophosphamide, ifosmide and mechlorethamine
Used in leukemia, lymphoma, breast cancer
SLE, MS, small vessel vasculitis
Nitrogen mustard can cause SIADH(water retention)
SE all AA bone marrow suppression, hair loss. GI problems, infertility, leukamia or other cancers, teratogenic
Cyclophosphamide
Prodrugs, forms carbonium with guanine N7
Acrolein (toxic metabolite)
Causes bladder cancer and hemorrhagic cystitis which can be prevented by fluid intake and use of SH donors eg mesna or sodium 2 mercaptoethane sulfonate
Busulfan
Not prodrug
Release methyl and highly toxic to bone marrow
Leukemia
Used before bone transplant to kill both cancer and healthy bones to make room for new one
SE pulmonary fibrosis, hyperpigmentation, bone marrow suppression
Procarbozine
It’s a monofunctional AA
Mechanism unknown
Hodgkin lymphoma and brain tumor
Avoid food rich in tyramine such as cheese, chocolate etc
SE cause leukamia, disulfiram like reaction, bone marrow suppression, pulmonary fibrosis