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20 Cards in this Set
- Front
- Back
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Why was there a need for second-generation platinum drugs?
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Cell may develop resistance to cisplatin: accumulation of cisplatin in the cell, to overcome the deactivation of cisplatin by metallothionein (sulfur-containing) and to overcome the cells increased ability ro repair DNA
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What are some side effects or symptoms of cisplatin?
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kidney damage (nephrotoxicity), nausea and vomiting, alopecia, myelosuppression (inhibited bone marrow production), ototoxicity (neural damage in the ear)
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What are the requirements for a platnium drug to be effective against cancer? [4]
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Platinum should have an oxidation state of II or IV
Complex should be neutral to pass through the cell membrane Complex must contain cis-leaving ligands (such as Cl- or oxygen) which can be replaced by water then DNA Complex should have unreactive, primary amine non-leaving ligands (NH3) which form hydrogen bonds with DNA |
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Carboplatin
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anti-cancer second-generation platinum drug which also reduced the risk of kidney damage (lung/ovarian cancer)
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Discuss the structure of carboplatin
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square planar complex with platinum (II), two cis-NH3 ligands, 5-membered bidentate chelate ring with an additional cyclobutane is the leaving ligand
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Is cisplatin a chelate? Why?
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No. There are no rings formed with the platinum, only monodentate Cl- and NH3
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Why is carboplatin less nephrotoxic?
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The bidentate cyclobutane-1,1-dicarboxylate ligand may slow down the degredation into damaging derivatives
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Oxaliplatin is used for
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a drug for colorectal cancer which is less prone to cell resistance from being more "chemically bulky"
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Discuss the structure of Oxaliplatin
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platinum (II) square planar complex with 2 bidentate chelate-ring ligands
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Gold forms stable compounds in +I and +III oxidation states. Which of these is toxic?
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Gold (III) complexes are toxic.
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What metal complexes are used for treating Rheumatoid Arthritis?
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Copper (II) complexes as well as copper bracelets.
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Discuss the chemistry of rheumatoid arthritis.
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Elevated copper levels in the caueruplasmin in the blood and reduced levels in the liver.
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How do copper bracelets work?
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The amino acids in sweat react with copper metal in the presence of oxygen making the copper cross through the skin.
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Relate between D-penicillamine and rheumatoid arthritis.
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D-pen activates the enzyme superoxide dismutase (SOD) which removes superoxide (a cause of joint inflamation)
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Discuss the relationship between Copper II in the body and rheumatoid arthritis
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In rheumatoid arthritis, there's an elevated level of copper-containing caeruloplasmin in the blood but a reduced level of copper in the liver.
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Caeruloplasmin
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the major copper-carrying protein in the blood; decreased levels in Wilson's disease and elevated levels in rheumatoid arthritis
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Myocrisin
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a gold-complex drug treatment for rheumatoid arthritis which has numerous toxic side effects
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Name 3 Gold (I) complex-ed drugs used for treating rheumatoid arthritis. Which is the only one which is orally active?
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Myocrisin & Solganal are injected intra-muscularly while auranofil is orally active
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How do Gold (I) complexes help in treating rheumatoid arthritis?
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The gold-complexes become concentrated in the inflamed joints and disrupt thiol cointaining enzymes which cause the inflammation
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Thiol group
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a -SH group
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