- Substituted (10H-phenothiazin-10-L)-propyl-1-piperazines
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Substituted (10H-phenothiazin-10-yl)propyl-1-piperazines of the formula STR1 wherein R1, R2, R3, A, X, m, n and s are as hereinafter set forth, are described. The compounds of formula I, which contain a piperazine moiety combined by an ether linkage to different phenolic moieties, are useful as orally active long lasting antipsychotic agents.
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- Potential CNS antitumor agents - Phenothiazines. II: Fluphenazine analogs
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Fluphenazine was found to possess moderate, reproducible activity against the intraperitoneal L-1210 and P-388 leukemia murine tumor models. Seven ether derivatives of fluphenazine and eight compounds in which the terminal side-chain hydroxyl group was replaced by an amine function were prepared and evaluated in the intraperitoneal L-1210, P-388, and B16 melanoma systems as well as the intracerebral L-1210 and ependymoblastoma brain tumor models. While no substantial intracerebral activity was observed, seven derivatives possessed reproducible activity in the intraperitoneal L-1210 or P-388 system. Several gave T/C [(treated survival/control survival) x 100%] values of 150%. No B16 melanoma activity was observed. These compounds were also tested for their cytototoxic properties in culture against L-1210, P-388, and KB cells. The amine isosteres, while possessing little in vivo activity, were the most cytotoxic of the compounds prepared, with several having ED50 values 1 μg/ml.
- Hirata,Peng,Driscoll
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p. 157 - 162
(2007/10/04)
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