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    Chemistry

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    Also known as: 6-thioguanine, 154-42-7, Tioguanine, 2-amino-6-mercaptopurine, 6-mercaptoguanine, Tioguanin
    Molecular Formula
    C5H5N5S
    Molecular Weight
    167.19  g/mol
    InChI Key
    WYWHKKSPHMUBEB-UHFFFAOYSA-N
    FDA UNII
    WIX31ZPX66
    Thioguanine
    An antineoplastic compound which also has antimetabolite action. The drug is used in the therapy of acute leukemia.
    Thioguanine anhydrous is an Antimetabolite.
    1 2D Structure

    Thioguanine

    2 Identification
    2.1 Computed Descriptors
    2.1.1 IUPAC Name
    2-amino-3,7-dihydropurine-6-thione
    2.1.2 InChI
    InChI=1S/C5H5N5S/c6-5-9-3-2(4(11)10-5)7-1-8-3/h1H,(H4,6,7,8,9,10,11)
    2.1.3 InChI Key
    WYWHKKSPHMUBEB-UHFFFAOYSA-N
    2.1.4 Canonical SMILES
    C1=NC2=C(N1)C(=S)N=C(N2)N
    2.2 Other Identifiers
    2.2.1 UNII
    WIX31ZPX66
    2.3 Synonyms
    2.3.1 MeSH Synonyms

    1. 2 Amino 6 Purinethiol

    2. 2-amino-6-purinethiol

    3. 6 Thioguanine

    4. 6-thioguanine

    5. Anhydrous, Thioguanine

    6. Lanvis

    7. Tabloid

    8. Thioguanin Gsk

    9. Thioguanin-gsk

    10. Thioguanine Anhydrous

    11. Thioguanine Hemihydrate

    12. Thioguanine Monosodium Salt

    13. Thioguanine Tabloid

    14. Thioguaningsk

    15. Tioguanina Wellcome

    16. Tioguanine

    2.3.2 Depositor-Supplied Synonyms

    1. 6-thioguanine

    2. 154-42-7

    3. Tioguanine

    4. 2-amino-6-mercaptopurine

    5. 6-mercaptoguanine

    6. Tioguanin

    7. Tabloid

    8. 2-amino-6-purinethiol

    9. Lanvis

    10. 2-amino 6mp

    11. 2-aminopurin-6-thiol

    12. 2-aminopurine-6-thiol

    13. 2-aminopurine-6(1h)-thione

    14. Wellcome U3b

    15. 6-mercapto-2-aminopurine

    16. 2-amino-9h-purine-6-thiol

    17. 6-tg

    18. 2-amino-6-merkaptopurin

    19. Tioguaninum

    20. Guanine, Thio-

    21. Tioguanina

    22. 6h-purine-6-thione, 2-amino-1,7-dihydro-

    23. 2-amino-1,7-dihydro-6h-purine-6-thione

    24. Thioguanine Anhydrous

    25. Nsc-752

    26. Bw 5071

    27. Purine-6-thiol, 2-amino-

    28. Purine-6(1h)-thione, 2-amino-

    29. 2-amino-1,9-dihydro-6h-purine-6-thione

    30. Tg

    31. Thioguanine, Anhydrous

    32. Thg

    33. Nsc 752

    34. 2-amino-1,7-dihydro-6h-purin-6-thion

    35. X 27

    36. Tioguanine (inn)

    37. Tioguanine [inn]

    38. 2-amino-6,7-dihydro-3h-purine-6-thione

    39. 2-amino-1,9-dihydropurine-6-thione

    40. Chembl727

    41. Wix31zpx66

    42. 2-amino-3,7-dihydro-6h-purine-6-thione

    43. Chebi:9555

    44. Nsc752

    45. Thioguanine2-amino-6-purinethiol

    46. 2-thioguanine

    47. 2-amino-1h-purine-6(9h)-thione

    48. 2-amino-1,7-dihydropurine-6-thione

    49. Nsc-76504

    50. Ncgc00094792-01

    51. Dsstox_cid_3652

    52. 2-amino-6-mp

    53. Tioguanine Hemihydrate

    54. Dsstox_rid_77129

    55. Dsstox_gsid_23652

    56. Tioguaninum [inn-latin]

    57. C5h5n5s

    58. 2-aminopurin-6-thiol [czech]

    59. Guanine, Thio- (van)

    60. 2-amino-6-merkaptopurin [czech]

    61. 6-tioguanine

    62. Tioguanina [inn-spanish]

    63. Cas-154-42-7

    64. Dx4

    65. Smr000857244

    66. Lanvis (tn)

    67. Ccris 8997

    68. 9h-purine-6-thiol, 2-amino-

    69. Hsdb 2504

    70. Sr-05000002077

    71. Einecs 205-827-2

    72. Thioguanine [usan:usp]

    73. 2-amino-1,7-dihydro-6h-purin-6-thion [czech]

    74. Unii-wix31zpx66

    75. Thioquanine

    76. Ai3-26078

    77. 6-thioguano-sine

    78. 6-tg/thioguanine

    79. Mfcd00233553

    80. 1330266-29-9

    81. Spectrum_000235

    82. Thioguanine [mi]

    83. Spectrum2_000695

    84. Spectrum3_000577

    85. Spectrum4_000926

    86. Spectrum5_001455

    87. Purine Antimetabolite: Antimetabolite: Inhibits Nucleic Acid Replication

    88. Thioguanine [hsdb]

    89. 2-amino-6-mercapto-purin

    90. 6-thioguanine, >=98%

    91. Schembl3701

    92. Schembl5898

    93. Nciopen2_004153

    94. Tioguanine [who-dd]

    95. Bspbio_001994

    96. Kbiogr_001452

    97. Kbiogr_002476

    98. Kbioss_000715

    99. Kbioss_002483

    100. Mls001333131

    101. Mls001333132

    102. Mls006010896

    103. Divk1c_000428

    104. Spectrum1500573

    105. Spbio_000849

    106. 154-42-7

    107. 6-thioguanine

    108. 2-amino-6-mercapto-9h-purine

    109. Gtpl6845

    110. Thioguanine (tn) (glaxosmith)

    111. Dtxsid6023652

    112. Hms501f10

    113. Kbio1_000428

    114. Kbio2_000715

    115. Kbio2_002476

    116. Kbio2_003283

    117. Kbio2_005044

    118. Kbio2_005851

    119. Kbio2_007612

    120. Kbio3_001494

    121. Kbio3_002954

    122. Cmap_000061

    123. Ninds_000428

    124. Bcpe000001

    125. Hms1921e09

    126. Hms2092m11

    127. Hms2235f05

    128. Hms3865g13

    129. Pharmakon1600-01500573

    130. Albb-023493

    131. Bcp27718

    132. Zinc6382803

    133. Tox21_111035

    134. Tox21_113184

    135. Tox21_202401

    136. Tox21_300275

    137. Bdbm50200099

    138. Ccg-39890

    139. Nsc757348

    140. S1774

    141. Akos003389499

    142. Akos015901298

    143. Tox21_111035_1

    144. 2-amino-1,7-dihydro-purine-6-thione

    145. 2-amino-1,9-dihydro-purine-6-thione

    146. Ac-8421

    147. Bcp9000197

    148. Ccg-213953

    149. Ccg-266338

    150. Cs-1497

    151. Db00352

    152. Nsc-757348

    153. Ps-5007

    154. Wln: T56 Bnm Fym Inj Fus Hz

    155. Idi1_000428

    156. Smp2_000326

    157. Ncgc00094792-02

    158. Ncgc00094792-03

    159. Ncgc00094792-05

    160. Ncgc00094792-06

    161. Ncgc00094792-17

    162. Ncgc00188976-01

    163. Ncgc00188976-02

    164. Ncgc00254082-01

    165. Ncgc00259950-01

    166. Ncgc00263442-01

    167. Ncgc00263442-02

    168. Ncgc00263442-05

    169. Ac-23020

    170. Bt166463

    171. Hy-13765

    172. Nci60_041643

    173. Smr004701808

    174. Sbi-0051533.p003

    175. Ft-0611217

    176. T0212

    177. 2-amino-1,7-dihydro-6h-purine-6-thione #

    178. C07648

    179. D08603

    180. T71841

    181. Ab00174074_06

    182. Ab00918694_06

    183. Ab01273926-01

    184. Ab01273926-02

    185. Ab01273926_03

    186. 154t427

    187. A809532

    188. Q385347

    189. Sr-05000002077-1

    190. Sr-05000002077-5

    191. W-108030

    192. W-205813

    193. Z2768769146

    194. 6-thioguanine;6-tg;2-amino-6-mercaptopurine;2-amino-6-purinethiol

    195. Thioguanine, United States Pharmacopeia (usp) Reference Standard

    196. Thioguanine;6-tg; 2-amino-6-mercaptopurine; 2-amino-6-purinethiol

    197. 6-thioguanine, Hybri-max(tm), 50 X, Gamma-irradiated, Lyophilized Powder, Bioxtra, Suitable For Hybridoma

    2.4 Create Date
    2005-03-25
    3 Chemical and Physical Properties
    Molecular Weight 167.19 g/mol
    Molecular Formula C5H5N5S
    XLogP3-0.1
    Hydrogen Bond Donor Count3
    Hydrogen Bond Acceptor Count2
    Rotatable Bond Count0
    Exact Mass167.02656635 g/mol
    Monoisotopic Mass167.02656635 g/mol
    Topological Polar Surface Area111 Ų
    Heavy Atom Count11
    Formal Charge0
    Complexity225
    Isotope Atom Count0
    Defined Atom Stereocenter Count0
    Undefined Atom Stereocenter Count0
    Defined Bond Stereocenter Count0
    Undefined Bond Stereocenter Count0
    Covalently Bonded Unit Count1
    4 Drug and Medication Information
    4.1 Drug Information
    1 of 2  
    Drug NameThioguanine
    PubMed HealthThioguanine (By mouth)
    Drug ClassesAntineoplastic Agent
    Drug LabelTABLOID brand Thioguanine was synthesized and developed by Hitchings, Elion, and associates at the Wellcome Research Laboratories. It is one of a large series of purine analogues which interfere with nucleic acid biosynthesis, and has been found acti...
    Active IngredientThioguanine
    Dosage FormTablet
    RouteOral
    Strength40mg
    Market StatusPrescription
    CompanyAspen Global

    2 of 2  
    Drug NameThioguanine
    PubMed HealthThioguanine (By mouth)
    Drug ClassesAntineoplastic Agent
    Drug LabelTABLOID brand Thioguanine was synthesized and developed by Hitchings, Elion, and associates at the Wellcome Research Laboratories. It is one of a large series of purine analogues which interfere with nucleic acid biosynthesis, and has been found acti...
    Active IngredientThioguanine
    Dosage FormTablet
    RouteOral
    Strength40mg
    Market StatusPrescription
    CompanyAspen Global

    4.2 Therapeutic Uses

    Antimetabolites, Antineoplastic

    National Library of Medicine's Medical Subject Headings online file (MeSH, 1999)

    CLINICALLY, THIOGUANINE HAS BEEN USED IN THE TREATMENT OF ACUTE LEUKEMIA AND, IN COMBINATION WITH CYTARABINE, IS ONE OF THE MOST EFFECTIVE AGENTS FOR INDUCTION OF REMISSIONS IN ACUTE GRANULOCYTIC LEUKEMIA; IT HAS NOT BEEN USEFUL IN THE TREATMENT OF PATIENTS WITH SOLID TUMORS. THIS CMPD HAS BEEN USED AS AN IMMUNOSUPPRESSIVE AGENT, PARTICULARLY IN PATIENTS WITH NEPHROSIS AND WITH COLLAGEN-VASCULAR DISORDERS. TOXIC MANIFESTATIONS INCLUDE BONE MARROW DEPRESSION AND GI EFFECTS, ALTHOUGH THE LATTER MAY BE LESS PRONOUNCED THAN WITH MERCAPTOPURINE.

    Gilman, A.G., T.W. Rall, A.S. Nies and P. Taylor (eds.). Goodman and Gilman's The Pharmacological Basis of Therapeutics. 8th ed. New York, NY. Pergamon Press, 1990., p. 1236

    SHORT TERM TREATMENT WITH DOXORUBICIN, CYTARABINE, & 6-THIOGUANINE WAS GIVEN TO 90 PATIENTS WITH ACUTE MYELOGENOUS LEUKEMIA. FIFTY PATIENTS RECEIVED HIGH DOSES (REGIMEN 1) & 41 RECEIVED VERY HIGH DOSES (REGIMEN 2). REMISSION RATE WAS SIGNIFICANTLY HIGHER WITH REGIMEN 1 THAN WITH REGIMEN 2. DURATION OF REMISSION WAS, HOWEVER, SIGNIFICANTLY LONGER WITH REGIMEN 2.

    BELL R ET AL; BR MED J 284 (APR 24): 221-24 (1982)

    IN ADVANCED COLORECTAL ADENOCARCINOMA, TWO DIFFERENT SCHEDULES OF COMBINATION METHYL-CCNU, 6-THIOGUANINE, & 5-FLUOROURACIL EXHIBITED SIMILAR EFFICACIES, WITH A COMBINED COMPLETE & PARTIAL REMISSION RATE OF 17% & A MEDIAN SURVIVAL OF 53+ WK. SIGNIFICANT SYMPTOMATIC BENEFIT WAS SEEN IN 52% OF PATIENTS. TOXICITY WAS PREDOMINATELY HEMOPOIETIC & GI.

    PMID:7231364 ARONEY RS ET AL; MED PEDIATR ONCOL 9 (2): 181-6 (1981)

    For more Therapeutic Uses (Complete) data for THIOGUANINE (14 total), please visit the HSDB record page.

    4.3 Drug Warning

    Risk-benefit should be considered when the following medical problems exist: Bone marrow depression; chickenpox, existing or recent (including recent exposure; herpes zoster (risk of severe generalized disease); gout, history of; urate renal stones, history of (risk of hyperuricemia); hepatic function impairment (reduced biotransformation; lower dosage is recommended); infection; renal function impairment (reduced elimination; lower dosage is recommended); or sensitivity to thioguanine. Caution should be used also in patients who have had cytotoxic drug therapy and radiation therapy within 4 to 6 weeks.

    USP Convention. USPDI-Drug Information for the Health Care Professional. 14th ed. Volume I. Rockville, MD: United States Pharmacopeial Convention, Inc., 1994. (Plus Updates)., p. 2653

    Because normal defense mechanisms may be suppressed by thioguanine therapy, concurrent use with alive virus vaccine may potentiate the replication of the vaccine virus, may increase the side/adverse effects of the vaccine virus, and/or may decrease the patient's antibody response to the vaccine; immunization of these patients should be undertaken only with extreme caution after careful review of the patient's hematologic status and only with the knowledge and consent of the physician managing the thioguanine therapy. The interval between discontinuation of medication that cause immunosuppression and restoration of the patient's ability to respond to the vaccine depends on the intensity and type of immunosuppression-causing medication used, the underlying disease, and other factors; estimates vary from 3 months to 1 year. Patients with leukemia in remission should not receive live virus vaccine until at least 3 months after their last chemotherapy. Immunization with oral poliovirus vaccine should also be postponed in persons in close contact with the patient, especially family members.

    USP Convention. USPDI-Drug Information for the Health Care Professional. 14th ed. Volume I. Rockville, MD: United States Pharmacopeial Convention, Inc., 1994. (Plus Updates)., p. 2653

    Because normal defense mechanisms may be suppressed by thioguanine therapy, the patient's antibody response to the vaccine may be decreased. The interval between discontinuation of medications that cause immunosuppression and restoration of the patient's ability to respond to the vaccine depends on the intensity and type of immunosuppression-causing medication used, the underlying disease, and other factors; estimates vary from 3 months to 1 year.

    USP Convention. USPDI-Drug Information for the Health Care Professional. 14th ed. Volume I. Rockville, MD: United States Pharmacopeial Convention, Inc., 1994. (Plus Updates)., p. 2653

    TOXIC MANIFESTATIONS INCL BONE MARROW DEPRESSION & GI EFFECTS ... .

    Gilman, A.G., T.W. Rall, A.S. Nies and P. Taylor (eds.). Goodman and Gilman's The Pharmacological Basis of Therapeutics. 8th ed. New York, NY. Pergamon Press, 1990., p. 1236

    For more Drug Warnings (Complete) data for THIOGUANINE (9 total), please visit the HSDB record page.

    4.4 Drug Indication

    For remission induction and remission consolidation treatment of acute nonlymphocytic leukemias.

    FDA Label

    5 Pharmacology and Biochemistry
    5.1 Pharmacology

    Thioguanine is an antineoplastic anti-metabolite used in the treatment of several forms of leukemia including acute nonlymphocytic leukemia. Anti-metabolites masquerade as purine or pyrimidine - which become the building blocks of DNA. They prevent these substances becoming incorporated in to DNA during the "S" phase (of the cell cycle), stopping normal development and division. Thioguanine was first synthesized and entered into clinical trial more than 30 years ago. It is a 6-thiopurine analogue of the naturally occurring purine bases hypoxanthine and guanine. Intracellular activation results in incorporation into DNA as a false purine base. An additional cytotoxic effect is related to its incorporation into RNA. Thioguanine is cross-resistant with mercaptopurine. Cytotoxicity is cell cycle phase-specific (S-phase).

    5.2 MeSH Pharmacological Classification

    Antimetabolites, Antineoplastic

    Antimetabolites that are useful in cancer chemotherapy. (See all compounds classified as Antimetabolites, Antineoplastic.)

    5.3 FDA Pharmacological Classification
    5.3.1 Active Moiety
    THIOGUANINE ANHYDROUS
    5.3.2 FDA UNII
    WIX31ZPX66
    5.3.3 Pharmacological Classes
    Antimetabolite [EPC]
    5.4 ATC Code

    L - Antineoplastic and immunomodulating agents

    L01 - Antineoplastic agents

    L01B - Antimetabolites

    L01BB - Purine analogues

    L01BB03 - Tioguanine

    5.5 Absorption, Distribution and Excretion

    Absorption

    Absorption of an oral dose is incomplete and variable, averaging approximately 30% of the administered dose (range: 14% to 46%)

    Incompletely and variably (about 30%) absorbed from the gastrointestinal tract.

    USP Convention. USPDI-Drug Information for the Health Care Professional. 14th ed. Volume I. Rockville, MD: United States Pharmacopeial Convention, Inc., 1994. (Plus Updates)., p. 2652

    THIOGUANINE IS INCOMPLETELY ABSORBED WHEN GIVEN ORALLY, AVERAGING ABOUT 30% OF AN ADMIN DOSE. ... THE ELIMINATION HALF-LIFE OF THE PARENT DRUG IS 1.5 HR, BUT PEAK PLASMA LEVELS OF METABOLITES ARE REACHED IN 6-8 HR. BETWEEN 24% & 46% IS EXCRETED IN THE URINE AS METABOLITES WITHIN 24 HR. ... THIS DRUG IS CLEARED RAPIDLY FROM PLASMA AFTER IV ADMINISTRATION; MORE THAN 80% EXCRETED WITHIN 24 HR. ALTHOUGH THIOGUANINE.../SRP: HAS LIMITED ACCESS ACROSS/ THE BLOOD-BRAIN BARRIER IN ANIMALS AFTER LARGE DOSES, VERY LITTLE ENTERS THE CEREBROSPINAL FLUID OF HUMANS AFTER THE USUAL CLINICAL DOSES ARE EMPLOYED.

    American Medical Association, Council on Drugs. AMA Drug Evaluations Annual 1994. Chicago, IL: American Medical Association, 1994., p. 2046

    THE METABOLISM AND PHARMACOKINETICS OF 6-THIOGUANINE WERE STUDIED IN DOGS AFTER IV ADMIN OF 5 MG/KG (35)S-THIOGUANINE (TG). THIOGUANINE WAS RAPIDLY & EXTENSIVELY DEGRADED. METABOLITES WERE NOT FOUND IN THE CEREBROSPINAL FLUID IN SIGNIFICANT CONCENTRATIONS.

    PMID:7307231 LOO TL ET AL; CANCER CHEMOTHER PHARMACOL 6 (2): 131-6 (1981)

    5.6 Metabolism/Metabolites

    Hepatic. First converted to 6-thioguanilyic acid (TGMP). TGMP is further converted to the di- and tri-phosphates, thioguanosine diphosphate (TGDP) and thioguanosine triphosphate (TGTP) by the same enzymes that metabolize guanine nucleotides.

    ... WHEN THIOGUANINE IS ADMIN TO MAN, THE S-METHYLATION PRODUCT, 2-AMINO-6-METHYLTHIOPURINE, RATHER THAN FREE THIOGUANINE APPEARS IN URINE; INORGANIC SULFATE IS ALSO A MAJOR URINARY METABOLITE. LESSER AMT OF 6-THIOURIC ACID ARE FORMED, SUGGESTING THAT DEAMINATION CATALYZED BY THE ENZYME GUANASE DOES NOT HAVE A MAJOR ROLE IN THE METABOLIC INACTIVATION OF THIOGUANINE.

    Gilman, A.G., T.W. Rall, A.S. Nies and P. Taylor (eds.). Goodman and Gilman's The Pharmacological Basis of Therapeutics. 8th ed. New York, NY. Pergamon Press, 1990., p. 1236

    THE PHARMACOKINETICS OF RADIOLABELED 6-THIOGUANINE (TG) WERE COMPARED WITH THAT OF BETA-2'-DEOXYTHIOGUANOSINE (BETA-TGDR) AFTER IV ADMIN. URINARY EXCRETION OF THE RADIOLABEL WAS 75% OF THE DOSE 24 HR AFTER ADMIN. BOTH THIOPURINES WERE RAPIDLY & EXTENSIVELY DEGRADED & EXCRETED AS 6-THIOXANTHINE, INORGANIC SULFATE, S-METHYL-6-THIOXANTHINE, & 6-THIOURIC ACID IN ADDITION TO OTHER PRODUCTS. SMALL AMOUNTS OF UNCHANGED DRUG WERE ALSO EXCRETED. STUDIES SUGGEST THAT BETA-TGDR IS A LATENT FORM OF TG. SINCE RESISTANCE TO ANTILEUKEMIC AGENT 6-THIOGUANINE INEVITABLY DEVELOPS IN ANIMAL TUMORS, THIS NEW AGENT BETA-TGDR IS OF POTENTIAL CLINICAL USE.

    LU K ET AL; PHARMACOKINETICS AND METABOLISM OF BETA-2'-DEOXYTHIOGUANOSINE AND 6-THIOGUANINE IN MAN; CANCER CHEMOTHER PHARMACOL 8 (1): 119-23 (1982)

    5.7 Biological Half-Life

    When the compound was given in singles doses of 65 to 300 mg/m^2, the median plasma half-disappearance time was 80 minutes (range 25-240 minutes)

    5.8 Mechanism of Action

    Thioguanine competes with hypoxanthine and guanine for the enzyme hypoxanthine-guanine phosphoribosyltransferase (HGPRTase) and is itself converted to 6-thioguanilyic acid (TGMP), which reaches high intracellular concentrations at therapeutic doses. TGMP interferes with the synthesis of guanine nucleotides by its inhibition of purine biosynthesis by pseudofeedback inhibition of glutamine-5-phosphoribosylpyrophosphate amidotransferase, the first enzyme unique to the de novo pathway of purine ribonucleotide synthesis. TGMP also inhibits the conversion of inosinic acid (IMP) to xanthylic acid (XMP) by competition for the enzyme IMP dehydrogenase. Thioguanine nucleotides are incorporated into both the DNA and the RNA by phosphodiester linkages, and some studies have shown that incorporation of such false bases contributes to the cytotoxicity of thioguanine. Its tumor inhibitory properties may be due to one or more of its effects on feedback inhibition of de novo purine synthesis; inhibition of purine nucleotide interconversions; or incorporation into the DNA and RNA. The overall result of its action is a sequential blockade of the utilization and synthesis of the purine nucleotides.

    THIOGUANINE, THE 6-THIO ANALOGUE OF GUANINE, IS A PRODRUG THAT IS CONVERTED TO 6-THIOGUANINE-RIBOSE-PHOSPHATE, AN ACTIVE METABOLITE. ... 6-THIOGUANINE-RIBOSE-PHOSPHATE IS A FEEDBACK INHIBITOR OF THE INITIAL (AMIDOTRANSFERASE) STEP IN PURINE BIOSYNTHESIS. THIS METABOLITE ALSO BLOCKS CONVERSIONS OF INOSINIC ACID TO GUANYLIC ACID & OF GUANYLIC ACID TO GDP. THIOGUANINE ALSO IS CONVERTED TO THE DEOXYNUCLEOTIDE TRIPHOSPHATE, WHICH CAN BE INCORPORATED INTO TUMOR CELL DNA. ALTHOUGH SOME INVESTIGATORS BELIEVE THAT THIS IS THE MAJOR MECHANISM OF CYTOTOXICITY, THE RELATIVE IMPORTANCE OF THE VARIOUS SITES OF ACTION HAS NOT BEEN DETERMINED. ... THIOGUANINE IS CELL-CYCLE SPECIFIC FOR THE S PHASE.

    American Medical Association, Council on Drugs. AMA Drug Evaluations Annual 1994. Chicago, IL: American Medical Association, 1994., p. 2046

    APPARENTLY, THE METABOLISM OF 6-THIOGUANINE TO 6-THIOGUANOSINE IN SARCOMA 180 & 180/TG CELLS IS MEDIATED BY PURINE NUCLEOSIDE PHOSPHORYLASE & NEWLY SYNTHESIZED 6-THIOGUANOSINE IS READILY EFFLUXED INTO THE CELLULAR ENVIRONMENT. THE FORMATION OF 6-THIOGUANINE, BY PURINE NUCLEOSIDE PHOSPHORYLASE, MAY BE IMPORTANT TO THE EXPRESSION OF CELLULAR SENSITIVITY TO 6-THIOGUANINE, IN THAT IT DECR THE AVAIL OF 6-THIOGUANINE FOR DIRECT CONVERSION BY HYPOXANTHINE-GUANINE PHOSPHORIBOSYLTRANSFERASE TO THE NUCLEOTIDE LEVEL, A PHENOMENON CRITICAL TO THE EXPRESSION OF THE ANTINEOPLASTIC ACTIVITY OF THE 6-THIOPURINES.

    PMID:7459851 LEE SH, SARTORELLI AC; CANCER RES 41 (3): 1086-90 (1981)

    PHENYL SUBSTITUTION AT C-8 OF 2-AMINO-6-MERCAPTOPURINE ABOLISHED THE IMMUNOSUPPRESSIVE ACTIVITY. THEREFORE, A NONSUBSTITUTED 8 POSITION OF 2-AMINO-6-MERCAPTOPURINE IS ESSENTIAL FOR IMMUNOSUPPRESSIVE ACTION.

    PMID:6031686 FU SC J ET AL; J MED CHEM 10 (1): 109-10 (1967)

    SPONTANEOUSLY CYCLING LYMPHOCYTES (IN CELL DIVISION IN CULTURES WITHOUT ADDITION OF PHYTOHEMAGGLUTININ, PHA) GO THROUGH VARIOUS PHASES OF 1ST DIVISION WITH THE SAME KINETICS AS PHA-STIMULATED CELLS. IN SAMPLES FROM 10 REFERENTS, THE FREQUENCY OF SPONTANEOUSLY CYCLING LYMPHOCYTES VARIED FROM 8.9X10-5 TO 9.5X10-3 AS INDICATED WITH AUTORADIOGRAPHY ON CELLS IN (S + G2) PHASE DETERMINED BY FLOW SORTING. IN PHA-STIMULATED SAMPLES FROM THE SAME PERSONS THE FREQUENCY OF 6-THIOGUANINE (TG)-RESISTANT VARIANTS WAS BETWEEN 4X10-7 & 2.6X10-6, WHICH INDICATES THAT MOST OF THE SPONTANEOUSLY CYCLING CELLS WERE TG-SENSITIVE.

    PMID:6690915 AMNEUS H ET AL; MUTAT RES 139 (1): 41-4 (1984)

    For more Mechanism of Action (Complete) data for THIOGUANINE (7 total), please visit the HSDB record page.

    API Reference Price

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