Against growth mixes/Antineoplastic Operators, section 38.


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Antimetabolites (Nucleoside Analogs, Folic corrosive analogs). Antimetabolites:Prevents blend of ordinary cell metabolitesOften close auxiliary likenesses metabolite and antimetaboliteearlier ex. PABA/sulfonamides. Nucleoside analogs as antimetabolitesPossible mecanisms:Incorporation DNA or RNA; misreadingInhibition of DNA polymeraseInhibition of KinasesInhib. of compounds included in pyrimidi
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Against disease mixes/Antineoplastic Agents, section 38 Cancer Therapy Surgery Radiation Immunologican Therapy ( interferons - Incr. nudge. Immune system microorganisms and B cells) Chemotherapy Alkylation Agents Antimetabolites/Nucleoside Analogs Antibiotics Antimitotic Agents Micellaneous Antineoplastic Agents Hormonal Therapy

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Antimetabolites (Nucleoside Analogs, Folic corrosive analogs) Antimetabolites: Prevents union of typical cell metabolites Often close auxiliary likenesses metabolite and antimetabolite earlier ex. PABA/sulfonamides

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Nucleoside analogs as antimetabolites Possible mecanisms: Incorporation DNA or RNA; misreading Inhibition of DNA polymerase Inhibition of Kinases Inhib. of proteins required in pyrimidine/purine biosynthesis

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5-Fluoruracil (5-FU) Fluorouracil®, Flurablastin®,

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Synth. thymine nucleotide from uracil nucleotide by thymidylate synthetase

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Kapecitabin Xelodar®, Additional systems: Incorp. DNA/RNA 5-FU digestion system Tegafur UFT®

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Cytarabine (ARA-C) Cytarabin®, Cytosar®, Gemcitasbin Gemzar®,

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6-Mercaptopurine (6-MP) Puri-Nethol®

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Fludarabine Fludara® Cladribin Leustatin®

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Potential Purine Antimetabolites

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Folic Acid analogs as antimetabolites Metotreksat Metoject® Raltitrexed Tomudex®

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Chemotherapy Alkylation Agents √ Antimetabolites/Nucleoside Analogs √ Antibiotics Antimitotic Agents Micellaneous Antineoplastic Agents Hormonal Therapy Metabolites from microorg., excessively dangerous as anti-microbials - anticancer comp. Bleomycins Actinomycins Mitomycins Antracyclins Coformycins

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Bleomycins Isolated from Streptomyces verticillius Naturally occuring as Cu-chelates 1) Binds Fe(II) inside cells 2) Bleomycin complexed Fe(II) diminish O 2 3) . Goodness radicals delivered 4) Cleavage of DNA Bleomycin Baxter®

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Actinomycins Isolated from Streptomyce s sp. Dactinomycin (Actinomycin D) Cosmegen®

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Quinolones Inhib DNA-union; DNA-gyrase (prokaryoter) uwounding DNA before replic.. DNA-topoisomerase (people), anticancer compds. ex. doxorubicin Unique mecanism, no cross resistance Broad range: G+ and G-; additionally mycobactria, clamydia

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Antracyclines Isolated Streptomyces sp , a few semisynth analogs Doxorubicin Doxorubicin® Adriamycin® Caelyx® R 1 = OMe, R 2 = OH, R 3 = H; R 4 = OH Daunorubicin Cerubidin® R 1 = OMe, R 2 = H, R 3 = H; R 4 = OH Epirubicin Farmorubicin® R 1 = OMe, R 2 = OH, R 3 = OH; R 4 = H Idarubicin Zavedos® R 1 = H, R 2 = H, R 3 = H; R 4 = OH Valrubicin Mitoxantrone Novantrone®

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Mechanism ≈ Actinomycins (Intercalation) Also collaborate aminosugar - phosphate Antraquinone - red/bull respond: prod. receptive oxygen radicals DNA-Daunomycin Complex

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Mitomycins Isolated Streptomyces sp , Mitomycin C Mutamycin®

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Conformycins Isolated Streptomyces sp , Also metab. of anticancer/antiviral adeninederiv. Geir Andresen Cytotox. Ex. move state analogs

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Chemotherapy Alkylation Agents √ Antimetabolites/Nucleoside Analogs √ Antibiotics √ Antimitotic Agents Micellaneous Antineoplastic Agents Hormonal Therapy

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Mitosis Prophase Metaphase Anaphase Telophase Antimitotic specialists tie to microtubuli Supression of microtubuli progression Metaphase capture

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Vinca alkaloids Vinca alkaloids (Indols) from Vinca rosea (Catharantus roseus) MadagaskarPerivinkle Binds to microtubuli - Supression of microtubuli elements Metaphase capture Depolymerization of microtubuli high conc.

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Taxanes First disengaged from bark of Western/Pacific yew ( Taxus brevifolia ) NIH screening of plant concentrates 1960s Mecanism ≈ Vinca alkaloids, distinctive restricting locales

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Palitaxel

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Availability Dried internal bark of Western/Pacific yew ( Taxus brevifolia ): 0.01 - 0.04% 1 kg Taxol - 900 kg bark (2000 - 3000 trees) - Other Taxus sp: Also palitaxel in needles (renewable source) - Semisynth from deacetylbaccatin III (0.1% in needles Taxus baccata ) (- Total combinations)

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Colchicine From Meadow-saffron, Colchicum autumnale (Tidløs) seeds Binds to microtubuli - metaphase capture, excessively harmful too be utilized as a part of growth treatment Used to treat gout (podagra)

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Comming next? - Epothilones Isolated from Myxobacteria (Epothilone A - F + synth. analogs)

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Chemotherapy Alkylation Agents √ Antimetabolites/Nucleoside Analogs √ Antibiotics √ Antimitotic Agents √ Micellaneous Antineoplastic Agents Hormonal Therapy Hydroxyurea Podophyllotoxines Camptothecins Compounds for photodynamic treatment Tyrosine-Kinase Inhibitors Hydroxykarbamid ® Inhib. ribonucleotide diphosphate reductase Arrest cells in G1-S interphase (combi with radiation)

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Podophyllotoxines From Podophyllum peltarum May apple Antiviral, veneric warts Toxic - lead for anticancer medications Etoposide Eposin® Etopofos® Vepesid® Affects DNA topoisomerase II (not intercalating) DNA strand breakage

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Camptothecins First segregated Camptotheca acuminata (Chinese tree) NIH screening Later found in a few plants Topotecan Hycamtin® Irinotecan Campto® Semisynth. inhib. DNA topoisomerase II, DNA strand breakage

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Compounds for photodynamic treatment Metylaminolevulinat Metvix® PhotoCure

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Tyrosine-Kinase Inhibitors

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Enzyme coupled receptors - Catalytic receptors (Chapter 4) Ligands: Peptide hormones

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Imatinib Glivec® Leukemia sorts Gefitinib Iressa® - Not in N. Lung growth Side impact: Intestinal lung sickness (might be lethal) 0.3 % US 2% Japan

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Chemotherapy Alkylation Agents √ Antimetabolites/Nucleoside Analogs √ Antibiotics √ Antimitotic Agents √ Micellaneous Antineoplastic Agents √ Hormonal Therapy

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Estrogens and agonists Antiestrogens Breast malignancy (estrogen depend.) Tamoxifen Nolvadex® Tamoxifen®

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Aromatase Inhibitors Estrogen depend. bosom disease Inhib. estrogen biosynth. Letrozol Femar® Exemestan Aromasin® Anastrosol Arimidex®

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Androgens Anti-androgens Flutamid Eulexin® Flutamid® Prostate disease Bicalutamid Casodex® Prostate malignancy (less tox.) 5 a - Reductase Inhibitors Finasterid Proscar® kind prostate

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