Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1983-05-19
1987-03-17
Hollrah, Glennon H.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
544315, 544316, 544318, 548540, 549 73, A61K 31505, C07D40306, C07D40506
Patent
active
046508007
ABSTRACT:
Compounds of the general formula: ##STR1## wherein X represents a halogen atom or a trifluoromethyl group; R.sup.1 represents a hydrogen atom or a lower alkyl group and Het represents an optionally substituted C-attached 5-7 membered aromatic heterocyclic ring which ring contains one or more heteroatoms selected from O, N and S and optionally carries a fused ring and where an acidic or basic group is present, the salts thereof have been found to possess excellent metaphase arresting ability and are of use in combating abnormal cell proliferation. Thus a knowledge of the cell division cycles of the normal and abnormal cells enables a cytotoxic drug to be administered while the abnormal cells are in a phase susceptible to attack and while the normal cells are in a non-susceptible phase.
The compounds of the invention are prepared by alkylation, deprotection of a protected keto group, oxidation or electrophilic halogenation.
REFERENCES:
Phillipps et al., "Chemical Abstracts", vol. 96, 1982, Cols. 181304c and 181305d.
Bain Brian M.
Borella Raymond A.
Phillipps Gordon H.
Steeples Ian P.
Williamson Christopher
Glaxo Group Limited
Hollrah Glennon H.
Turnipseed James H.
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