[Quantitative aspects of the relationship of the antitumor activity and toxicity of diaziridinyl-sym. triazines to their physicochemical properties]. 1979

B A Ivin, and V A Filov, and B O Kraĭz, and V V Belogorodskiĭ, and L L Maliugina

The experiments on rats have shown that there is a linear dependence of the logarithms of reciprocal molar toxic (LD50) and therapeutic (ED50) for sarcoma 45 doses of 6-oxyalkyl-amino-2,4-bis(I-aziridinyl)-sym-triazines and 6-(5-substituted-2,2-dimethyl-1,3-dioxan-5-yl)-amino-2,4-bis(I-aziridinyl)-sym-triazines upon the induction constants of substituents at tertiary carbon, the antitumor activity being more sensitive to the substituent effect compared with the toxicity. The dependence of the logarithms of reciprocal molar therapeutic (ED50 for sarcoma 45 and ED95 for Walker sarcoma) and toxic (LD50 and LD100) doses of the compounds, both synthesized by us and taken from the literature, upon the logarithms of their distribution coefficients in the octanol-water system (IgP) shows a parabolic character with the maximum effect at the extreme point of the parabola. The antitumor activity was more sensitive to a changed IgP than the toxicity.

UI MeSH Term Description Entries
D007928 Lethal Dose 50 The dose amount of poisonous or toxic substance or dose of ionizing radiation required to kill 50% of the tested population. LD50,Dose 50, Lethal
D002279 Carcinoma 256, Walker A transplantable carcinoma of the rat that originally appeared spontaneously in the mammary gland of a pregnant albino rat, and which now resembles a carcinoma in young transplants and a sarcoma in older transplants. (Stedman, 25th ed) Carcinosarcoma 256, Walker,Walker Carcinoma 256,Walker Carcinosarcoma 256
D002627 Chemistry, Physical The study of CHEMICAL PHENOMENA and processes in terms of the underlying PHYSICAL PHENOMENA and processes. Physical Chemistry,Chemistries, Physical,Physical Chemistries
D004305 Dose-Response Relationship, Drug The relationship between the dose of an administered drug and the response of the organism to the drug. Dose Response Relationship, Drug,Dose-Response Relationships, Drug,Drug Dose-Response Relationship,Drug Dose-Response Relationships,Relationship, Drug Dose-Response,Relationships, Drug Dose-Response
D004353 Drug Evaluation, Preclinical Preclinical testing of drugs in experimental animals or in vitro for their biological and toxic effects and potential clinical applications. Drug Screening,Evaluation Studies, Drug, Pre-Clinical,Drug Evaluation Studies, Preclinical,Drug Evaluations, Preclinical,Evaluation Studies, Drug, Preclinical,Evaluation, Preclinical Drug,Evaluations, Preclinical Drug,Medicinal Plants Testing, Preclinical,Preclinical Drug Evaluation,Preclinical Drug Evaluations,Drug Screenings,Screening, Drug,Screenings, Drug
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D000970 Antineoplastic Agents Substances that inhibit or prevent the proliferation of NEOPLASMS. Anticancer Agent,Antineoplastic,Antineoplastic Agent,Antineoplastic Drug,Antitumor Agent,Antitumor Drug,Cancer Chemotherapy Agent,Cancer Chemotherapy Drug,Anticancer Agents,Antineoplastic Drugs,Antineoplastics,Antitumor Agents,Antitumor Drugs,Cancer Chemotherapy Agents,Cancer Chemotherapy Drugs,Chemotherapeutic Anticancer Agents,Chemotherapeutic Anticancer Drug,Agent, Anticancer,Agent, Antineoplastic,Agent, Antitumor,Agent, Cancer Chemotherapy,Agents, Anticancer,Agents, Antineoplastic,Agents, Antitumor,Agents, Cancer Chemotherapy,Agents, Chemotherapeutic Anticancer,Chemotherapy Agent, Cancer,Chemotherapy Agents, Cancer,Chemotherapy Drug, Cancer,Chemotherapy Drugs, Cancer,Drug, Antineoplastic,Drug, Antitumor,Drug, Cancer Chemotherapy,Drug, Chemotherapeutic Anticancer,Drugs, Antineoplastic,Drugs, Antitumor,Drugs, Cancer Chemotherapy
D001388 Aziridines Saturated azacyclopropane compounds. They include compounds with substitutions on CARBON or NITROGEN atoms. Ethyleneimines,Azacyclopropanes, Saturated,Dimethyleneimines,Saturated Azacyclopropanes
D001389 Azirines Unsaturated azacyclopropane compounds that are three-membered heterocycles of a nitrogen and two carbon atoms. Azacyclopropanes, Unsaturated,Unsaturated Azacyclopropanes
D012513 Sarcoma, Experimental Experimentally induced neoplasms of CONNECTIVE TISSUE in animals to provide a model for studying human SARCOMA. EHS Tumor,Sarcoma, Engelbreth-Holm-Swarm,Sarcoma, Jensen,Experimental Sarcoma,Experimental Sarcomas,Sarcomas, Experimental,Engelbreth-Holm-Swarm Sarcoma,Jensen Sarcoma,Sarcoma, Engelbreth Holm Swarm,Tumor, EHS

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