Term
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Definition
| loss of CL leads to intramolecular cyclization of side chain leads to reactive ethylene immonium derivative |
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Term
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Definition
| broad spectrum of activity |
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Term
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Definition
| alkylating agents, platinums |
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Term
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Definition
| Alkylate DNA but carbamylate proteins (lisine residues) which leads to toxicity; can pass blood brain barrier |
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Term
| non-classical alkylating agents; temosolomide, decarbazine, procarbazine |
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Definition
| N-methylated by liver microsomal enzymes, then function as an alkylating agent; methylates Guanine and Adenosine |
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Term
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Definition
| cross-link DNA; intrastrand (same strand of two-strand double helix) and interstrand (opposite strands of double helix), monoalkylate and intermediate |
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Term
| Platinum analogs (cisplatin, carboplatin) |
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Definition
| Cl dissociates creating a reactive complex that reacts with water and interacts with DNA leading to inTRAstrand cross-linking (G N7 with adjaccent G O6) ultimately causing denaturation DNA |
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Term
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Definition
| folic acid analogs, pyrimidine analogs, and purine analogs |
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Term
| folic acid analogs examples |
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Definition
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Term
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Definition
| competitively inhibits dihydrofolate reductase (FH2 Reductase); inhibits one carbon transfer which allows |
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Term
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Definition
| converts DUMP to DTMP, taking the one carbon unit (methyl group) from FH4 which oxidates into FH2 |
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Term
| Florouracil converted to FDUMP |
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Definition
| inhibits thymidylate synthetase |
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Term
| pyrimidine analogs of cytosine, thymine and uracil |
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Definition
| incorporation into DNA/RNA; misreading, inhibition of DNA polymerase; inhibiting DNA elongation, inhibition of kinases, inhibition of enzymes involved in pyrimidine biosynthesis |
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Term
| DNA polymerase inhibitors |
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Definition
| pyrimidine analogs (cytarabine in particular), fludarabine |
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Term
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Definition
| prodrug; hydroxylation leads to haldol phosphamide, then alkylation of guanine residue |
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Term
| phsphoramide mustard and acrolein (toxic) |
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Definition
| metabolites of cyclophosphamide |
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Term
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Definition
| inside tumor cells, it is activated to a "fraudulent" nucleotide |
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Term
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Definition
| prodrug; phosphorylated in vivo to ara CTP which completely inhibits DNA polymerase and blocks synthesis causing cell death |
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Term
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Definition
| active metabolite of cytarabine that competes with dCTP and inhibits DNA polymerase, incorporates into DNA producing strand breaks AND triggers apoptosis |
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Term
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Definition
| 6-MP, 6-TG and fludarabine |
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Term
| 6-MP, 6-TG and fludarabine |
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Definition
| prodrug; must be converted to nucleotides, MUST occur in target cells, rapidly broken down to inactive products but nucleotide forms have longer half-lives |
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Term
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Definition
| must be converted intracellularly to nucleoside by HGPRT |
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Term
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Definition
| dephosphorylated to 2-fluoro-arabinofluranosyladenosine then phosphorylated intracellularly to TP |
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Term
| anthracycline; daunorubacine, doxorubacin, mitoxantrone |
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Definition
| intercalate into the base pairs in DNA minor groove, inhibit topoisomerase II preventing relaxation of supercoiled DNA, free radical damage of cell membrane |
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Term
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Definition
| reduced and reacts with amino acid groups on guanine residues on adjacent base pairs in complementary DNA strands that result in cross-linking |
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Term
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Definition
| planar end of bleomycin molecule intercalates with DNA (between GT and GC) sequence, the other end binds to Fe and facilitate its oxidation to Fe which generates oxygen free radicals |
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Term
| vinka alkyloids; vincristine and vinblastine |
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Definition
| binds to tubulin diamers in cytoplasm which inhibits ASSEMBLY of microtubules causing an arrest of M phase |
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Term
| taxanes; paclitaxel and docetaxel |
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Definition
| disrupt equilibrium between free tubulin and microtubules by shifting it in the direction of assembly; inhibits DISASSEMBLY of microtubules leading to abnormal bundles of microtubules |
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Term
| camptothecins; topotecan, irinotecan |
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Definition
| binds to DNA/ topo I which creates a cleavable complex preventing DNA re-ligation leading to DNA damage (single strand breaks) during S-phase |
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Term
| epipodopyllotoxins; etoposide or VP-16 |
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Definition
| forms ternary complex complex with DNA and topo II leading to the formation of cleavable complex which causes DNA damage (double stranded breakage) and cell death |
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Term
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Definition
| topo II inhibitor; anthracycling and epipodopyllotoxins |
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Term
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Definition
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