medicinal chemistry 3 final

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rockjst
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medicinal chemistry 3 final
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2014-12-04 19:55:11
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medicinal chemistry
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medchem 3 final
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  1. nitrogen mustards cross-link _____ DNA strands
    separate
  2. nitrogen mustard derived from L-Phe
    melphalan
  3. nitrogen mustard.  beta-oxidation metabolite is active
    chlorambucil
  4. nitrogen mustard with weak alkylating effects.  works primarily by inhibiting mitosis.  used in palliative treatment of prostate cancers
    estramustine
  5. metabolite of some nitrogen mustards that is uro/nephrotoxic
    acrolein
  6. metabolite of some nitrogen mustards that is nephro/neurotoxic
    chloroacetaldehyde
  7. essentially a soluble mercapto group.  given with cyclophosphamide to minimize bladder toxicity
    mesna
  8. acrolein can alkylate _____ residues in bladder cells
    Cys
  9. iphosphamide has higher metabolism to _____ than cyclophosphamide, leading to higher toxicities
    acrolein
  10. mustard alkylators require _____ dosing
    high, intermittent
  11. active species of nitrosureas that can carbamylate Lys
    isocyanate
  12. DNA-alkylating active species of nitrosureas
    2-chloroethyl carbocation
  13. highly lipophilic nitrosurea.  administered IV/wafer.  used in brain and blood cancers
    carmustine
  14. orally available nitrosurea used in brain tumors and hodgkins.  watch for seizures if wafers are used
    lomustine
  15. nitrosurea used exclusively in metastatic islet cell pancreatic carcinoma.  highly nephrotoxic--monitor kidney function
    streptozocin
  16. procarbazines/triazines act via ______
    O6-methylation of guanine nucleotides
  17. active species of procarbazines and triazines.  potent methylator.  causes guanine to pair with thymine
    diazomethane
  18. used for hodgkins, extensively cleared hepatically. inhibits monoamine oxidase and ethanol metabolism
    procarbazine hcl
  19. prodrug administered IV for malignant melanoma.  potent emesis-induction.  forty percent excreted unchanged
    dacarbazine
  20. orally available prodrug used for glioblastoma and astrocytoma.  same active metabolite as dacarbazine.  myelosuppression and alopecia common.  food strongly decreases absorption
    temozolamide
  21. temozolamide, unlike dacarbazine has _____
    no CYP-required activation
  22. major urinary metabolite of dacarbazine and temozolamide.  seems to interfere with purine synthesis
    AIC
  23. triazine derivative that works via degredation to formaldehyde (DNA-protein cross-linking).  use is restricted no non-organoplatinum-responsive ovarian cancer.  peripheral neuropathy is a unique side effect.
    altretamine
  24. activity is limited to bone marrow.  causes hyperuricemia.  used in chronic myelogenous leukemia.  works similarly to mustards by N-alyklating DNA bases and alternatively by alkylating SH groups in cysteine or glutathione
    busulfan
  25. importantly, organoplatinums alkylate _____, mostly guanine, more rarely adenine
    adjacent bases most commonly intrastrand
  26. ammonia ligands stabilize a bent DNA complex by interacting with _____
    phosphate groups of the DNA backbone
  27. administered IV.  reacts with Al. rapidly hydrated.  used for metastatic testicular/ovarian or advanced bladder cancer. highly nephrotoxic.  sodium thiosulfate can neutralize it in the kidneys and diuretics can be given.  highly protein bound.  potent emetogen and peculiarly, ototoxicity.
    cisplatin
  28. less potent and longer halflife than cisplatin.  unlike cisplatin, it is also used for lung, head, and neck cancers.  milder AEs than cisplatin.  same active species, slower kinetics.
    carboplatin
  29. diaquo form is active species.  has a bulky moiety that extends into DNA major grooves.  improved selectivity and efficacy. pulminary fibrosis and neuropathies are possible.  used in metastatic colon and rectal cancer alone or with 5-FU
    oxaliplatin
  30. investigational Pt(IV) complex with six metabolites.  main active species contains Pt(II)--desacetoxy.  used investigationally in prostate cancer, and maybe ovarian and SCLC
    satraplatin

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