Structural requirements for biological activity among antileukemic glaucarubolone ester quassinoids. 1976

S M Kupchan, and J A Lacadie, and G A Howie, and B R Sickles

A C-15 ester substituent is required for significant antileukemic activity among the glaucarubolone ester quassinoids, and variations in the ester group are not accompanied by particularly marked changes in antileukemic activity. Unsaturation at the 3,4 position is advantageous for optimal activity, and hydrogenation of this double bond results in marked diminution in both cytotoxicity toward KB cells in tissue culture and inhibitory activity against the P-388 lymphocytic leukemia in mice.

UI MeSH Term Description Entries
D007942 Leukemia, Experimental Leukemia induced experimentally in animals by exposure to leukemogenic agents, such as VIRUSES; RADIATION; or by TRANSPLANTATION of leukemic tissues. Experimental Leukemia,Experimental Leukemias,Leukemia Model, Animal,Leukemias, Experimental,Animal Leukemia Model,Animal Leukemia Models,Leukemia Models, Animal
D011714 Pyrans Pyran
D002460 Cell Line Established cell cultures that have the potential to propagate indefinitely. Cell Lines,Line, Cell,Lines, Cell
D005900 Glaucarubin (1 beta,2 alpha,11 beta,12 alpha,15 beta(S))-11,20-Epoxy-1,2,11,12-tetrahydroxy-15-(2-hydroxy-2-methyl-1-oxobutoxy)picras-3-en-16-one. A quassinoid (Simaroubolide) from Simaruba glauca, a tropical shrub. It has been used as an antiamebic agent and is found to be cytotoxic. It may be of use in cancer chemotherapy. Kirondrin
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
D013329 Structure-Activity Relationship The relationship between the chemical structure of a compound and its biological or pharmacological activity. Compounds are often classed together because they have structural characteristics in common including shape, size, stereochemical arrangement, and distribution of functional groups. Relationship, Structure-Activity,Relationships, Structure-Activity,Structure Activity Relationship,Structure-Activity Relationships
D051379 Mice The common name for the genus Mus. Mice, House,Mus,Mus musculus,Mice, Laboratory,Mouse,Mouse, House,Mouse, Laboratory,Mouse, Swiss,Mus domesticus,Mus musculus domesticus,Swiss Mice,House Mice,House Mouse,Laboratory Mice,Laboratory Mouse,Mice, Swiss,Swiss Mouse,domesticus, Mus musculus

Related Publications

S M Kupchan, and J A Lacadie, and G A Howie, and B R Sickles
January 1978, Journal of medicinal chemistry,
S M Kupchan, and J A Lacadie, and G A Howie, and B R Sickles
December 1978, Journal of medicinal chemistry,
S M Kupchan, and J A Lacadie, and G A Howie, and B R Sickles
May 1974, Journal of the American Chemical Society,
S M Kupchan, and J A Lacadie, and G A Howie, and B R Sickles
April 1980, Biochemical and biophysical research communications,
S M Kupchan, and J A Lacadie, and G A Howie, and B R Sickles
January 1995, Proceedings of the Society for Experimental Biology and Medicine. Society for Experimental Biology and Medicine (New York, N.Y.),
S M Kupchan, and J A Lacadie, and G A Howie, and B R Sickles
January 1994, Peptides,
S M Kupchan, and J A Lacadie, and G A Howie, and B R Sickles
June 1968, Nutrition reviews,
S M Kupchan, and J A Lacadie, and G A Howie, and B R Sickles
January 1999, Zeitschrift fur Naturforschung. C, Journal of biosciences,
S M Kupchan, and J A Lacadie, and G A Howie, and B R Sickles
October 1985, Archives of biochemistry and biophysics,
S M Kupchan, and J A Lacadie, and G A Howie, and B R Sickles
January 1992, International journal of peptide and protein research,
Copied contents to your clipboard!