Telomerase inhibitors

Details Telomerase inhibitors Telomerase inhibitors

1995-10-06

1998-06-16

Ivy, C. Warren

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

546288, 514335, 514344, A61K 3144, C07D40112, C07D21332, C07D21385

Patent

active

057672784

ABSTRACT:
Compounds for treating cancer and other diseases involving telomerase activity are characterized by the following structure: ##STR1## Such compounds include those for which X.sub.1 is oxygen, sulfur, sulfone, or sulfinyl, and R.sub.1 is --Y.sub.n R.sub.6, where n is an integer between 0 and 10 and each Y.sub.n independently is methylene, methine, or quaternary carbon. R.sub.6, is alkyl, aryl, heteroaryl, aralkyl, or heteroaralkyl, alkylcarbonyl, arylcarbonyl, heteroalkylcarbonyl, heteroaralkylcarbonyl, aralkylcarbonyl, arninocarbonyl, alkylarninocarbonyl, arylaminocarbonyl, dialkylaminocarbonyl, diarylaminocarbonyl, arylalkylaminocarbonyl, carboxyl, carboxaldehyde, alkoxycarbonyl, aryloxycarbonyl, sulfo, alkylsulfonyl, arylsulfonyl, alkylsulfinyl, or arylsulfinyl. R.sub.6 can also be a linker selected from the group consisting of alkyl, aryl, and heterocycle. R.sub.2 is hydrogen, alkyl, aryl, hydroxyl, alkoxyl, aryloxyl, halogen, cyano, amino, alkylamino, arylamino, dialkylamino, diarylamino, arylalkylamino, aminocarbonyl, alkylaminocarbonyl, arylaminocarbonyl, dialkylaminocarbonyl, diarylaminocarbonyl, arylalkylaminocarbonyl, alkylcarbonyl, arylcarbonyl, alkylcarbonyloxy, arylcarbonyloxy, carboxyl, alkoxycarbonyl, aryloxycarbonyl, sulfo, alkylsulfonyl, or arylsulfonyl. R.sub.3 and R.sub.4 independently can be hydrogen, amino, alkylamino, arylamino, heterocycleamino, aralkylamino, dialkylamino, diarylamino, heterocylcealkylamino, alkylcarbonyl, arylcarbonyl, nitro, halogen, hydroxyl, aryloxyl, alkoxyl, lower alkyl, aryl, heteroaryl, aralkyl, cyano, carboxyl, alkoxycarbonyl, aryloxycarbonyl, aralkoxycarbonyl, or heteroaralkyl. R.sub.5 is selected from the group consisting of iminyl, hydroximinyl, alkyliminyl, aryliminyl, aralkyliminyl, alkoximinyl, aryloximinyl, heterocycleiminyl, and cyclic iminyl. Provided, however, that R.sub.5 is not 4-methylphenyliminyl when X.sub.1 is sulfur, n is 1, Y is methylene, R.sub.2 is cyano, R.sub.3 and R.sub.4 are hydrogen, and R.sub.6 is 4-chlorophenyl.

REFERENCES:
patent: 4269846 (1981-05-01), Huang et al.
patent: 4611059 (1986-09-01), Sih
patent: 4863923 (1989-09-01), Ho et al.
Steven L. Castle et al., "The Synthesis of 1103-1108 (1987).
David T. Connor et al., "Novel Benzothiophene-, Benzofuran-, and Naphthalenecarboxamidotetrazoles as Potential Antiallergy Agents," Journal of Medicinal Chemistry, vol. 35, No. 5, pp. 958-965 (1992).
Tatsuo Higa and Arnold J. Krubsack, "Oxidations by Thionyl Chloride. 8. A Ketones," J. Org. Chem., vol. 41, No. 21, pp. 3399-3403 (1976).
Tatsuo Higa and Arnold J. Krubsack, "Oxidations By Thionyl Chloride, VI. Mechanism of the Reaction with Cinnamic Acids," J. Org. Chem, vol. 40, No. 21, pp. 3037-3045 (1975).
Nam W. Kim et al., "Specific Association of Human Telomerase Activity with Immortal Cells and Cancer," Science vol. 266, pp. 2011-2014 (1994). Liebigs Ann. Chem, pp. 1424-1427 (1980).

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