Abstract
Bis (1-aziridinyl)(hexahydro-1H-azepin-1-yl)phosphine sulfide, an active anticancer agent with low hematopoietic toxicity in animals and man, was recommended several years ago for breast cancer adjuvant chemotherapy as an alternate drug to thiotepa. This hope had led to the syntheses of aziridinylallylaminophosphine oxides or sulfides (compounds I-XVII) in our laboratories. The resurgent interest in this area of cancer chemotherapy encouraged us to report our synthetic work as well as their evaluation as both anticancer agents and insect chemosterilants. Based on observed antitumor activity in animals, low chemosterilant activity in female species (insects and rats), and histochemical observation of tissue toxicity in rat testes but not in ovaries, these new agents are of potential interest to the breast cancer adjuvant chemotherapy program.
Publication types
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Research Support, U.S. Gov't, Non-P.H.S.
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Animals
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Antineoplastic Agents / chemical synthesis*
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Antineoplastic Agents / therapeutic use
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Aziridines / chemical synthesis
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Aziridines / pharmacology
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Aziridines / therapeutic use
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Carcinoma 256, Walker / drug therapy
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Chemosterilants
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Female
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Fertility / drug effects
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Houseflies
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Infertility, Male / chemically induced
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Leukemia L1210 / drug therapy
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Male
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Mice
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Organophosphorus Compounds / chemical synthesis*
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Organophosphorus Compounds / pharmacology
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Organophosphorus Compounds / therapeutic use
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Organothiophosphorus Compounds / chemical synthesis
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Organothiophosphorus Compounds / pharmacology
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Organothiophosphorus Compounds / therapeutic use
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Rats
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Structure-Activity Relationship
Substances
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Antineoplastic Agents
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Aziridines
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Chemosterilants
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Organophosphorus Compounds
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Organothiophosphorus Compounds