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Christopher Michejda

Research Profile

Chemicals & Drugs

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Alkylation

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Sergey G Tarasov; Yuhong Chen; Marzena A Dyba; Vadim Gaponenko; O M Zack Howard; Youngshim Lee; Christopher J Michejda; Joost J Oppenheim; Sriram Subramaniam; Nadya I Tarasova
Structural plasticity of a transmembrane peptide allows self-assembly into biologically active nanoparticles.
Susan K Keay; Piotr Kaczmarek; Chen-Ou Zhang; Kristopher Koch; Zoltan Szekely; Joseph J Barchi; Christopher J Michejda
Normalization of proliferation and tight junction formation in bladder epithelial cells from patients with interstitial cystitis/painful bladder syndrome by d-proline and d-pipecolic acid derivatives of antiproliferative factor.
Ulrike Muus; Curtis Hose; Wei Yao; Teresa Kosakowska-Cholody; David Farnsworth; Marzena Dyba; George T Lountos; David S Waugh; Anne Monks; Terrence R Burke; Christopher J Michejda
Development of antiproliferative phenylmaleimides that activate the unfolded protein response.

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All Publications

2011: Sergey G Tarasov; Yuhong Chen; Marzena A Dyba; Vadim Gaponenko; O M Zack Howard; Youngshim Lee; Christopher J Michejda; Joost J Oppenheim; Sriram Subramaniam; Nadya I Tarasova
Structural plasticity of a transmembrane peptide allows self-assembly into biologically active nanoparticles.
Proceedings of the National Academy of Sciences of the United States of America 2011;108(24):9798-803.
2011: Susan K Keay; Piotr Kaczmarek; Chen-Ou Zhang; Kristopher Koch; Zoltan Szekely; Joseph J Barchi; Christopher J Michejda
Normalization of proliferation and tight junction formation in bladder epithelial cells from patients with interstitial cystitis/painful bladder syndrome by d-proline and d-pipecolic acid derivatives of antiproliferative factor.
Chemical biology & drug design 2011;77(6):421-30.
2010: Ulrike Muus; Curtis Hose; Wei Yao; Teresa Kosakowska-Cholody; David Farnsworth; Marzena Dyba; George T Lountos; David S Waugh; Anne Monks; Terrence R Burke; Christopher J Michejda
Development of antiproliferative phenylmaleimides that activate the unfolded protein response.
Bioorganic & medicinal chemistry 2010;18(12):4535-41.
2009: Teresa Kosakowska-Cholody; Wieslaw Cholody; Humcha K Hariprakasha; Anne Monks; Siddhartha Kar; Meifang Wang; Christopher J Michejda; Brian I Carr
Growth inhibition of hepatocellular carcinoma cells in vitro and in vivo by the 8-methoxy analog of WMC79.
Cancer chemotherapy and pharmacology 2009;63(5):769-78.
2008: Piotr Kaczmarek; Susan K Keay; Gillian Tocci; Kristopher R Koch; Chen-Ou Zhang; Joseph J Barchi; David Grkovic; Li Guo; Christopher J Michejda
Structure-activity relationship studies for the peptide portion of the bladder epithelial cell antiproliferative factor from interstitial cystitis patients.
Journal of medicinal chemistry 2008;51(19):5974-83.
2008: Terry W Moody; Tapas Pradhan; Samuel A Mantey; Robert T Jensen; Marcin Dyba; Deborah Moody; Nadya I Tarasova; Christopher J Michejda
Bombesin marine toxin conjugates inhibit the growth of lung cancer cells.
Life sciences 2008;82(15-16):855-61.
2007: Olga Timofeeva; Vadim Gaponenko; Stephen J Lockett; Sergey G Tarasov; Sheng Jiang; Christopher J Michejda; Alan O Perantoni; Nadya I Tarasova
Rationally designed inhibitors identify STAT3 N-domain as a promising anticancer drug target.
ACS chemical biology 2007;2(12):799-809.
2007: Peng Li; Sheng Jiang; Sheau-Ling Lee; Chen-Yong Lin; Michael Johnson; Robert B Dickson; Christopher J Michejda; Peter P Roller
Design and synthesis of novel and potent inhibitors of the type II transmembrane serine protease, matriptase, based upon the sunflower trypsin inhibitor-1.
Journal of medicinal chemistry 2007;50(24):5976-83.
2007: Humcha K Hariprakasha; Teresa Kosakowska-Cholody; Colin Meyer; Wieslaw Cholody; Sherman F Stinson; Nadya I Tarasova; Christopher J Michejda
Optimization of naphthalimide-imidazoacridone with potent antitumor activity leading to clinical candidate (HKH40A, RTA 502).
Journal of medicinal chemistry 2007;50(23):5557-60.
2007: Peng Li; Sheng Jiang; Stephanie C Pero; Lyn Oligino; David N Krag; Christopher J Michejda; Peter P Roller
Design and synthesis of paclitaxel conjugated with an ErbB2-recognizing peptide, EC-1.
Biopolymers 2007;87(4):225-30.
2007: Marshall L Morningstar; Thomas Roth; David W Farnsworth; Marilyn Kroeger Smith; Karen Watson; Robert W Buckheit; Kalyan Das; Wanyi Zhang; Eddy Arnold; John G Julias; Stephen H Hughes; Christopher J Michejda
Synthesis, biological activity, and crystal structure of potent nonnucleoside inhibitors of HIV-1 reverse transcriptase that retain activity against mutant forms of the enzyme.
Journal of medicinal chemistry 2007;50(17):4003-15.
2007: Deborah L Moody; Marcin Dyba; Teresa Kosakowska-Cholody; Nadya I Tarasova; Christopher J Michejda
Synthesis and biological activity of 5-aza-ellipticine derivatives.
Bioorganic & medicinal chemistry letters 2007;17(8):2380-4.
2006: Thomas P Conrads; Gillian Tocci; Brian L Hood; Chen-Ou Zhang; Li Guo; Kristopher R Koch; Christopher J Michejda; Timothy D Veenstra; Susan K Keay
CKAP4/p63 is a receptor for the frizzled-8 protein-related antiproliferative factor from interstitial cystitis patients.
The Journal of biological chemistry 2006;281(49):37836-43.
2006: Siddhartha Kar; Meifang Wang; Wei Yao; Christopher J Michejda; Brian I Carr
PM-20, a novel inhibitor of Cdc25A, induces extracellular signal-regulated kinase 1/2 phosphorylation and inhibits hepatocellular carcinoma growth in vitro and in vivo.
Molecular cancer therapeutics 2006;5(6):1511-9.
2005: Teresa Kosakowska-Cholody; Wieslaw Cholody; Anne Monks; Barbara Woynarowska; Christopher J Michejda
WMC-79, a potent agent against colon cancers, induces apoptosis through a p53-dependent pathway.
Molecular cancer therapeutics 2005;4(10):1617-27.
2005: Wieslaw Cholody; Teresa Kosakowska-Cholody; Melinda G Hollingshead; Humcha K Hariprakasha; Christopher J Michejda
A new synthetic agent with potent but selective cytotoxic activity against cancer.
Journal of medicinal chemistry 2005;48(13):4474-81.
2005: Nadya I Tarasova; Rishi Seth; Sergey G Tarasov; Teresa Kosakowska-Cholody; Christine A Hrycyna; Michael M Gottesman; Christopher J Michejda
Transmembrane inhibitors of P-glycoprotein, an ABC transporter.
Journal of medicinal chemistry 2005;48(11):3768-75.
2004: Terry W Moody; Gregory Czerwinski; Nadya I Tarasova; Deborah L Moody; Christopher J Michejda
The development of VIP-ellipticine conjugates.
Regulatory peptides 2004;123(1-3):187-92.
2004: Huiyun Liang; Richard Salinas; Belinda Z Leal; Teresa Kosakowska-Cholody; Christopher J Michejda; Stephen J Waters; Terence S Herman; Jan Woynarowski; Barbara Woynarowska
Caspase-mediated apoptosis and caspase-independent cell death induced by irofulven in prostate cancer cells.
Molecular cancer therapeutics 2004;3(11):1385-96.
2004: Susan K Keay; Zoltan Szekely; Thomas P Conrads; Timothy D Veenstra; Joseph J Barchi; Chen-Ou Zhang; Kristopher R Koch; Christopher J Michejda
An antiproliferative factor from interstitial cystitis patients is a frizzled 8 protein-related sialoglycopeptide.
Proceedings of the National Academy of Sciences of the United States of America 2004;101(32):11803-8.
2004: Marcin Dyba; Nadya I Tarasova; Christopher J Michejda
Small molecule toxins targeting tumor receptors.
Current pharmaceutical design 2004;10(19):2311-34.
2003: Sergey G Tarasov; Jose R Casas-Finet; Wieslaw Cholody; Teresa Kosakowska-Cholody; Zygmunt Gryczynski; Christopher J Michejda
Bisimidazoacridones: 2. Steady-state and time-resolved fluorescence studies of their diverse interactions with DNA.
Photochemistry and photobiology 2003;78(4):313-22.
2003: Marilyn B Kroeger Smith; Brian M Hose; Arie Hawkins; James Lipchock; David W Farnsworth; Robert C Rizzo; Julian Tirado-Rives; Eddy Arnold; Wanyi Zhang; Stephen H Hughes; William L Jorgensen; Christopher J Michejda; Richard H Smith
Molecular modeling calculations of HIV-1 reverse transcriptase nonnucleoside inhibitors: correlation of binding energy with biological activity for novel 2-aryl-substituted benzimidazole analogues.
Journal of medicinal chemistry 2003;46(10):1940-7.
2003: Marilyn B Kroeger Smith; Sandra Ruby; Stanislav Horouzhenko; Bryan Buckingham; Julia Richardson; Ina O'Carroll; Emily Potts; William L Jorgensen; Eddy Arnold; Wanyi Zhang; Stephen H Hughes; Christopher J Michejda; Richard H Smith
HIV-1 reverse transcriptase variants: molecular modeling of Y181C, V106A, L100I, and K103N mutations with nonnucleoside inhibitors using Monte Carlo simulations in combination with a linear response method.
Drug design and discovery 2003;18(4):151-63.
2002: T W Moody; Gregory Czerwinski; Nadya I Tarasova; Christopher J Michejda
VIP-ellipticine derivatives inhibit the growth of breast cancer cells.
Life sciences 2002;71(9):1005-14.
2001: Wieslaw Cholody; Teresa Kosakowska-Cholody; Christopher J Michejda
Bisimidazoacridones induce a potent cytostatic effect in colon tumor cells that sensitizes them to killing by UCN-01.
Cancer chemotherapy and pharmacology 2001;47(3):241-9.
2000: Marilyn B Kroeger Smith; ML Lamb; Julian Tirado-Rives; William L Jorgensen; Christopher J Michejda; S K Ruby; Richard H Smith
Monte Carlo calculations on HIV-1 reverse transcriptase complexed with the non-nucleoside inhibitor 8-Cl TIBO: contribution of the L100I and Y181C variants to protein stability and biological activity.
Protein engineering 2000;13(6):413-21.
1999: Nadya I Tarasova; W G Rice; Christopher J Michejda
Inhibition of G-protein-coupled receptor function by disruption of transmembrane domain interactions.
The Journal of biological chemistry 1999;274(49):34911-5.
1999: Sergey G Tarasov; Jose R Casas-Finet; Wieslaw Cholody; Christopher J Michejda
Bisimidazoacridones: effect of molecular environment on conformation and photophysical properties.
Photochemistry and photobiology 1999;70(4):568-78.
1998: Richard H Smith; William L Jorgensen; Julian Tirado-Rives; ML Lamb; Paul A J Janssen; Christopher J Michejda; Marilyn B Kroeger Smith
Prediction of binding affinities for TIBO inhibitors of HIV-1 reverse transcriptase using Monte Carlo simulations in a linear response method.
Journal of medicinal chemistry 1998;41(26):5272-86.
1998: Gregory Czerwinski; Nadya I Tarasova; Christopher J Michejda
Cytotoxic agents directed to peptide hormone receptors: defining the requirements for a successful drug.
Proceedings of the National Academy of Sciences of the United States of America 1998;95(20):11520-5.
1998: O M Zack Howard; T Korte; Nadya I Tarasova; M Grimm; Jim A Turpin; W G Rice; Christopher J Michejda; R Blumenthal; Joost J Oppenheim
Small molecule inhibitor of HIV-1 cell fusion blocks chemokine receptor-mediated function.
Journal of leukocyte biology 1998;64(1):6-13.
1998: Nadya I Tarasova; RH Stauber; Christopher J Michejda
Spontaneous and ligand-induced trafficking of CXC-chemokine receptor 4.
The Journal of biological chemistry 1998;273(26):15883-6.
1998: Jim A Turpin; Robert W Buckheit; D Derse; Melinda G Hollingshead; K Williamson; C Palamone; MC Osterling; S A Hill; L Graham; CA Schaeffer; M Bu; M Huang; Wieslaw Cholody; Christopher J Michejda; William G Rice
Inhibition of acute-, latent-, and chronic-phase human immunodeficiency virus type 1 (HIV-1) replication by a bistriazoloacridone analog that selectively inhibits HIV-1 transcription.
Antimicrobial agents and chemotherapy 1998;42(3):487-94.
1998: Nadya I Tarasova; Gregory Czerwinski; N B Roberts; J Lubkowski; T L Sumpter; B N Green; Christopher J Michejda
Mass spectrometry as a tool for studying the action of human aspartic proteases on peptides and proteins.
Advances in experimental medicine and biology 1998;436():201-6.
1997: T Roth; M L Morningstar; Paul L Boyer; S H Hughes; Robert W Buckheit; Christopher J Michejda
Synthesis and biological activity of novel nonnucleoside inhibitors of HIV-1 reverse transcriptase. 2-Aryl-substituted benzimidazoles.
Journal of medicinal chemistry 1997;40(26):4199-207.
1997: Marilyn B Kroeger Smith; Christopher J Michejda; Stephen H Hughes; Paul L Boyer; Paul A J Janssen; Koen Andries; Robert W Buckheit; Richard H Smith
Molecular modeling of HIV-1 reverse transcriptase drug-resistant mutant strains: implications for the mechanism of polymerase action.
Protein engineering 1997;10(12):1379-83.
1997: Nadya I Tarasova; RH Stauber; J K Choi; E A Hudson; Gregory Czerwinski; J L Miller; George Pavlakis; Christopher J Michejda; Stephen A Wank
Visualization of G protein-coupled receptor trafficking with the aid of the green fluorescent protein. Endocytosis and recycling of cholecystokinin receptor type A.
The Journal of biological chemistry 1997;272(23):14817-24.
1997: Nadya I Tarasova; Stephen A Wank; E A Hudson; V I Romanov; Gregory Czerwinski; James Resau; Christopher J Michejda
Endocytosis of gastrin in cancer cells expressing gastrin/CCK-B receptor.
Cell and tissue research 1997;287(2):325-33.
1996: Kalyan Das; J Ding; Y Hsiou; Arthur D Clark; HE Moereels; L Koymans; Koen Andries; R Pauwels; Paul A J Janssen; Paul L Boyer; P Clark; Richard H Smith; Marilyn B Kroeger Smith; Christopher J Michejda; Stephen H Hughes; Eddy Arnold
Crystal structures of 8-Cl and 9-Cl TIBO complexed with wild-type HIV-1 RT and 8-Cl TIBO complexed with the Tyr181Cys HIV-1 RT drug-resistant mutant.
Journal of molecular biology 1996;264(5):1085-100.
1996: M B Smith; B F Schmidt; Gregory Czerwinski; Lisa Anne Taneyhill; E J Snyder; A M Kline; Christopher J Michejda; Richard H Smith
Specificity of DNA alkylation by 1-(2-chloroethyl)-3-alkyl-3-acyltriazenes depends on the structure of the acyl group: kinetic and product studies.
Chemical research in toxicology 1996;9(2):466-75.
1996: Marilyn B Kroeger Smith; Lisa Anne Taneyhill; Christopher J Michejda; Richard H Smith
Base sequence selectivity in the alkylation of DNA by 1,3-dialkyl-3-acyltriazenes.
Chemical research in toxicology 1996;9(1):341-8.
1996: C A Rouzer; M Sabourin; T L Skinner; E J Thompson; T O Wood; G N Chmurny; J R Klose; J M Roman; Richard H Smith; Christopher J Michejda
Oxidative metabolism of 1-(2-chloroethyl)-3-alkyl-3- (methylcarbamoyl)triazenes: formation of chloroacetaldehyde and relevance to biological activity.
Chemical research in toxicology 1996;9(1):172-8.
1996: Nadya I Tarasova; V I Romanov; P P Da Silva; Christopher J Michejda
Numerous cell targets for gastrin in the guinea pig stomach revealed by gastrin/CCKB receptor localization.
Cell and tissue research 1996;283(1):1-6.
1995: Wieslaw Cholody; L Hernandez; L Hassner; Dominic A Scudiero; D B Djurickovic; Christopher J Michejda
Bisimidazoacridones and related compounds: new antineoplastic agents with high selectivity against colon tumors.
Journal of medicinal chemistry 1995;38(16):3043-52.
1995: L Hernandez; Wieslaw Cholody; E A Hudson; James Resau; G Pauly; Christopher J Michejda
Mechanism of action of bisimidazoacridones, new drugs with potent, selective activity against colon cancer.
Cancer research 1995;55(11):2338-45.
1994: B F Schmidt; L Hernandez; C Rouzer; Gregory Czerwinski; G Chmurny; Christopher J Michejda
Peptide-linked 1,3-dialkyl-3-acyltriazenes: gastrin receptor directed antineoplastic alkylating agents.
Journal of medicinal chemistry 1994;37(22):3812-8.
1994: Christopher J Michejda; M B Kroeger Koepke
Carcinogen activation by sulfate conjugate formation.
Advances in pharmacology (San Diego, Calif.) 1994;27():331-63.
1994: Christopher J Michejda; R H Smith; M B Kroeger Koepke
DNA alkylation by triazenes and related compounds.
IARC scientific publications 1994;(125):323-37.
1993: C A Rouzer; E J Thompson; T L Skinner; P A Heavner; W P Bartolini; K Mitchell; E Kurz; Richard H Smith; Christopher J Michejda
An unexpected pathway for the metabolic degradation of 1,3-dialkyl-3-acyltriazenes.
Biochemical pharmacology 1993;46(1):165-73.
1992: M B Kroeger-Koepke; Christopher J Michejda; R H Smith
Alkylation of DNA by 1,3-dialkyl-3-acyltriazenes: correlation of biological activity with chemical behavior.
Chemical research in toxicology 1992;5(4):541-7.
1992: M B Kroeger-Koepke; S R Koepke; L Hernandez; Christopher J Michejda
Activation of a beta-hydroxyalkylnitrosamine to alkylating agents: evidence for the involvement of a sulfotransferase.
Cancer research 1992;52(12):3300-5.
1991: M B Kroeger-Koepke; R H Smith; E A Goodnow; J Brashears; L Kratz; A W Andrews; W G Alvord; Christopher J Michejda
1,3-Dialkyltriazenes: reactive intermediates and DNA alkylation.
Chemical research in toxicology 1991;4(3):334-40.
1991: Christopher J Michejda
Carcinogenic consequences of DNA alkylation.
Contributions to gynecology and obstetrics 1991;18():71-8.
1991: S R Koepke; M B Kroeger-Koepke; Christopher J Michejda
Mechanism of DNA binding by the oesophageal carcinogen N-nitroso-N-methylaniline.
IARC scientific publications 1991;(105):346-50.
1990: Larry K Keefer; M B Kroeger-Koepke; H Ishizaki; Christopher J Michejda; Joseph E Saavedra; Joseph A Hrabie; Chung S Yang; P P Roller
Stereoselectivity in the microsomal conversion of N-nitrosodimethylamine to formaldehyde.
Chemical research in toxicology 1990;3(6):540-4.
1990: R H Smith; Dominic A Scudiero; Christopher J Michejda
1,3-Dialkyl-3-acyltriazenes, a novel class of antineoplastic alkylating agents.
Journal of medicinal chemistry 1990;33(9):2579-83.
1990: S R Koepke; M B Kroeger-Koepke; Christopher J Michejda
Evidence for an unstable DNA adduct from N-nitroso-N-methylaniline.
Chemical research in toxicology 1990;3(1):17-20.
1988: S R Koepke; M B Kroeger-Koepke; W Bosan; B J Thomas; W G Alvord; Christopher J Michejda
Alkylation of DNA in rats by N-nitrosomethyl-(2-hydroxyethyl)amine: dose response and persistence of the alkylated lesions in vivo.
Cancer research 1988;48(6):1537-42.
1988: S R Koepke; D R Creasia; G L Knutsen; Christopher J Michejda
Carcinogenicity of hydroxyalkylnitrosamines in F344 rats: contrasting behavior of beta- and gamma-hydroxylated nitrosamines.
Cancer research 1988;48(6):1533-6.
1987: S R Koepke; M B Kroeger-Koepke; Christopher J Michejda
N-nitroso-N-methylaniline: possible mode of DNA modification.
IARC scientific publications 1987;(84):68-70.
1987: Christopher J Michejda; S R Koepke; M B Kroeger-Koepke; W Bosan
Recent findings on the metabolism of beta-hydroxyalkylnitrosamines.
IARC scientific publications 1987;(84):77-82.
1986: Christopher J Michejda; M B Kroeger-Koepke; R M Kovatch
Carcinogenic effects of sequential administration of two nitrosamines in Fischer 344 rats.
Cancer research 1986;46(5):2252-6.
1985: S R Koepke; Y Tondeur; J G Farrelly; M L Stewart; Christopher J Michejda; M B Kroeger-Koepke
Metabolic studies of 15N-labeled N-nitrosoproline in isolated rat hepatocytes and subcellular fractions.
Cancer letters 1985;27(3):277-83.
1985: M B Kroeger-Koepke; Christopher J Michejda; P P Roller; Larry K Keefer
Use of 3,4-dichlorobenzenethiol as a trapping agent for alkylating intermediates during in vitro metabolism of nitrosamines.
Cancer research 1985;45(7):2973-5.
1984: S R Koepke; Y Tondeur; J G Farrelly; M L Stewart; Christopher J Michejda; M B Kroeger-Koepke
Metabolism of 15N-labelled N-nitrosodimethylamine and N-nitroso-N-methylaniline by isolated rat hepatocytes.
Biochemical pharmacology 1984;33(9):1509-13.
1984: S R Koepke; M B Kroeger-Koepke; Y Tondeur; J G Farrelly; M Stewart; Christopher J Michejda
alpha-Hydroxylation of nitrogen-15 labelled N-nitrosamines by isolated hepatocytes.
IARC scientific publications 1984;(57):437-42.
1983: M B Kroeger-Koepke; M D Reuber; P T Iype; W Lijinsky; Christopher J Michejda
The effect of substituents in the aromatic ring on carcinogenicity of N-nitrosomethylaniline in F344 rats.
Carcinogenesis 1983;4(2):157-60.
1982: Christopher J Michejda; S R Koepke
O-alkylation of N-nitrosamines. Transalkylation of N-nitrosamines and formation of electrophilic intermediates.
IARC scientific publications 1982;(41):451-7.
1981: M B Kroeger-Koepke; S R Koepke; G A McClusky; P N Magee; Christopher J Michejda
alpha-Hydroxylation pathway in the in vitro metabolism of carcinogenic nitrosamines: N-nitrosodimethylamine and N-nitroso-N-methylaniline.
Proceedings of the National Academy of Sciences of the United States of America 1981;78(10):6489-93.
1981: M B Kroeger-Koepke; A W Andrews; R J Kupper; S R Koepke; Christopher J Michejda
Mutagenicity and rat-liver S9 demethylation kinetics of N-nitrosomethylaniline and its ring-substituted derivatives.
Mutation research 1981;89(4):255-67.
1980: D H Sieh; A W Andrews; Christopher J Michejda
Mutagenicity of trialkyltriazenes: mutagenic potency of alkyldiazonium ions, the putative ultimate carcinogens from dialkylnitrosamines.
Mutation research 1980;73(2):227-35.
1980: R Kupper; M D Reuber; B N Blackwell; W Lijinsky; S R Koepke; Christopher J Michejda
Carcinogenicity of the isomeric, N-nitroso-delta3-and N-nitroso-delta2-piperidines in rats and the in vivo isomerization of the delta3-to the delta2-isomer.
Carcinogenesis 1980;1(9):753-7.
1980: Christopher J Michejda; S R Koepke; R Kupper
Formation and chemistry of alpha- and beta-oxidized nitrosamines.
IARC scientific publications 1980;(31):155-67.