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See LKT's Specialty Chemicals |
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See LKT's Product Line |
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LKT Laboratories, Inc. is the holder of the following patents. All LKT patents
are available for licensing. Please contact us for more details.
1-800-LKT-LABS or danrick@lktlabs.com |
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| Organoselenium Compounds for Cancer Chemoprevention |
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US Patent No. 6,703,524 B2 |
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US Patent No. 7,087,639 B2 |
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US Patent No. 7,314,929 B2 |
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| Heterocyclic Compounds for Cancer Chemoprevention |
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US Patent No. 6,166,003 |
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Phenylbutyl isothiocyanate (PBITC) is an inhibitor of chemically-induced lung carcinogenesis (1). n-Butyl thiophene (BT) inhibits colon carcinogenesis (2). LKT Laboratories has designed thienylbutyl isothiocyanate (TBITC) to incorporate the active functional groups of isothiocyanate in PBITC and thiophene in BT to achieve the inhibitory activities of both compounds (3). We refer to such compounds as “bifunctional inhibitors”, where the term “bifunctional” refers to the the two biologically active functional groups present in the compound.
The activity of TBITC has been confirmed by three prescreening assays: the induction of glutathione-S-transferase, the inhibition of lung methylation, and reduction of colon aberrant crypts formation3. Bioassays with lung and colon tumor models indicate that TBITC is an effective cancer chemopreventive agent in both target tissues. Structure activity relationship studies of phenyl-alkyl isothiocyanates have shown that there is a preference for longer alkyl chain lengths in the prevention of 4- (methylnitrosamino)-1-(3-pyridyl)-1-butanone (NNK)-induced lung tumors, with a six carbon chain being the most effective (4). Against esophageal tumors induced by Nnitrosomethylamylamine (NMAA), an ethyl group is the most effective (5). Benzyl isothiocyanate, but not phenylethyl isothiocyanate, inhibits benzo[a]pyrene-induced lung tumors(6). To promote similar SAR studies with thienyl alky isothiocyanates, LKT Labs offers the full series from thienylmethyl isothiocyanate (n = 1) to thienyl decyl iso-thiocyanate (n = 10), plus thienyl dodecyl isothiocyanate (n = 12). This series of bifunctional inhibitors of chemical carcinogenesis represents a new and novel class of chemopreventive agents. |
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| U.S. Patent No. |
6,703,524 B2 |
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| U.S. Patent No. |
6,166,003 |
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1. Sung, HJ., Choi, SM., et al. Experimental & Molecular Medicine. 31(4):174-8 (1999).
1. Morse, M.A., Eklind, K.I., Amin, S.G., Hecht, S.S. and Chung, F.-L. Carcinogenesis, 10:1757-9 (1989).
2. Lam, L.K., and Zhang, J. Carcinogenesis, 12:2311-5 (1995).
3. Lam, L.K.T., Kenney, P., Bergstrom, C.P. and Lam, S.H. Proc. Amer. Assoc. Cancer Res., 40:57 (1999).
4. Jiao, D., Smith, T.J., Yang, C.S., et al. Carcinogenesis, 18:2143-7 (1997).
5. Huang, Q., Lawson, T.A., Chung, F.L., Morris, C.R. and Mervish, S.S. Carcinogenesis, 14:749-54 (1993).
6. Lin, J.M., Amin, S., Trushin, N. and Hecht, S.S. Cancer Lett. 74:151-9 (1993). |
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