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Med Chem Exam 5 - Antitumor Antibiotics
Terms in this set (73)
___________ agents are "flat compounds" that bind strongly to DNA by slipping between two sets of base pairs in the double helix
Intercalating agents inhibit ___________.
Intercalating agent produced by streptomyces parvulus
Which intercalating agent has a peptide-lactone system?
Dactinomycin's (lactone/tricyclic) component inserts into the (major/minor) groove of DNA.
At high doses, dactinomycin inhibits all but:
a. RNA synthesis
b. protein synthesis
c. DNA synthesis
d. folylpolyglutamyl synthetase
Inhibition of RNA synthesis requires much (higher/lower) dactinomycin concentration than that for inhibition of DNA synthesis
The _______ moiety of some intercalating agents produces reactive oxygen species
The (sugar/anthraquinone) moiety of doxorubicin and daunorubicin produces oxygen free radicals; these can be severely cardiotoxic
The (sugar/anthraquinone) moiety of doxorubicin and daunorubicin intercalate into DNA base pairs
The anthraquinone moiety of doxorubicin and daunorubicin intercalate into DNA base pairs in the (major/minor) groove
Doxorubicin and daunorubicin produce DNA single strand breaks and inhibit repair. Which of the following is NOT a theory of their mechanism of action?
a. they produce free radicals
b. they inhibit dihydrofolate reductase
c. they "nick" DNA
d. they inhibit topoisomerase II
The two anthracycline intercalating agents are ___________ and __________.
CYP 450 Reductase and ______ shuttle a single electron between doxorubicin and oxygen during redox cycling.
True or false: Mitoxantrone is less cardiotoxic than doxorubicin.
What drug in this unit causes a delayed transit through the S-phase?
True or false: Mitoxantrone is an intercalating agent and inhibits topoisomerase II
True or false: Etoposide is an intercalating agent
Cells are most sensitive to etoposide in what phases?
Etoposide is thought to work inhibiting topoisomerase II and also by blocking the proper functioning of the:
c. Golgi apparatus
d. Na+/K+ ATPases
What enzymes manage the configuration of the DNA helix?
A group of glycoproteins produced by streptomyces verticillius
Bleomycins are administered as a mix of all but which of the following:
a. bleomycin B1-4
b. bleomycin A2
c. bleomycin AI2
d. bleomycin C8
Iron +2 is oxidized to Iron +3 in the mechanism of which drug?
The bleomycins transfer an electron from
Fe++ to O2 to produce __________.
Which of the following produces superoxide?
b. mitomycin C
e. they all produce superoxide
Bleomycin is most toxic in which tissues?
______ are much more effective at inhibiting DNA synthesis than RNA synthesis. They also cause cells to accumulate in the G2 phase.
True or false: Bleomycins cause strand scission and fragmentation of DNA -- both single and double strand breaks.
(scission is a fancy word for "breakage" as far as I can tell)
Bleomycin is contraindicated in patients over 50 with _______ disease
Produced by streotomyces caespitosus; a bifunctional molecule that can crosslink AND form damaging free radicals
True or False: Mitomycin can form crosslinks
Which of the following is not one of the functional groups in mitomycin that causes cell damage?
a. Perhalo ketone
Mitomycin C generates free radicals when it is reduced from the quinone to the ___________.
True or false: Mitomycin is a prodrug
(it has to get reduced to the hydroquinone to be active)
The molecule on the (left/right) is the hydroquinone form of mitomycin
The molecule on the (left/right) is hydroquinone
The molecule on the (left/right) is the quinone
Mitomycin forms crosslinks by bonding with the O6 and N2 of guanine and N6 of ______.
DNA attacks the (aziridinium/hydroquinone) ion in Mitomycin
2 drugs derived from a periwinkle plant
__________ and ________ cause dissolution of spindles during metaphase
Vincristine and vinblastine cause dissolution of the spindles during _________.
Vincristine, vinblastine, and paclitaxol stop cell division at ____phase.
Vincristine and vinblastine (promote/inhibit) the polymerization of tubulin molecules
Comes from a yew tree
Paclitaxel is also known as
Paclitaxel side chain at C__ is essential for activity
(Docletaxil/paclitaxel) is more potent
Paclitaxel promotes microtubule (formation/dissolution)
Vincristine & vinblastine promote microtubule (formation/dissolution)
Paclitaxel prevents microtubule (formation/disassembly)
paclitaxel resistance is due to cells making (more/less) p-glycoproteins
(p-glycoproteins force harmful molecules out of cells)
What forms covalent bonds with DNA but is not an alkylating agent?
If cisplatin is dissolved in water, the equilibrium shifts to the (left/right)
If cisplatin is dissolved in sea water, the equilibrium shifts to the (left/right)
Hydrolysis is (faster/slower) in D5W than in normal saline.
True or false: Cisplatin will bind to all bases, but most strongly with adenine
Pick the best solvent for cisplatin (assuming you want it to have the highest cytotoxicity possible):
1. 0.9% NaCl in water
2. 1/2 normal saline
3. Bacteriostatic H2O
_________ tumors are most sensitive to cisplatin
Cisplatin forms (inter/intra)strand crosslinks
antitumor agents that cause dissolution of the spindles (microtubles), stopping cell division at metaphase (cytostatic)
vincristine and vinblastine are indole alkaloids isolated from
"Catharantus roseus" (periwinkle) aka Vinca rosa
antitumor agent isolated from the bark of "Taxus brevifolia," aka Western yew or Pacific yew
present in vinca alkaloids: vincristine, vinblastine
cisplatin is the most stable in which solution:
-most stable in NS because the Cl- pushes the equilibrium to the left (as opposed to the hydrated form)
(D5W < 1/2NS < NS)
Organoplatinim complex that binds to DNA as a bidentate complex. Will bind to all bases, but most strongly with guanine
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