Abstract: There are provided novel anti-leukemic epoxides which are isolated from Baccharis megapotamica. The novel compounds are characterized by a 12,13-epoxytrichothecene central ring system which is spanned by a dienic macrolide ester side chain. The active compounds are characterized by the presence of an oxygen atom in the A-ring which takes the form of either a beta hydroxy group in the 8 position together with an unsaturated bond at the 9: 10 position or, alternatively, an epoxide group lying between the 9 and 10 position. Compounds devoid of either of these groups show no anti-leukemic activity.The active compounds possess high and surprising anti-leukemic activity against P-388 lymphocytic leukemia in in vivo assays in mice.

Abstract: There is disclosed a novel and improved method of synthesizing aporphines utilizing the Pschorr cyclization of 1-(2'-aminobenzyl)-7 hydroxy-1,2,3,4-tetrahydroisoquinolines in place of the corresponding 7-methoxy compounds.In the novel process of the present invention the amino group is diazotized and cyclized in the presence of copper powder.

Abstract: There are provided novel diterpenoid triepoxides, derived from Tripterygium wilfordii Hook F. which possess high and surprising antileukemic activity at dosage levels of micrograms/kilogram body weight.

Abstract: There is disclosed a novel total synthesis of Thalicarpine which includes inter alia a total synthesis of hernandaline. The novel process is characterized in utilizing simple and readily available starting materials to form a diaryl ether system which is then condensed with a 3,4-dihydroisoquinolinium salt which is then converted to hernandaline. Hernandaline is reacted with a bicyclic Reissert compound to yield a compound having the thalicarpine skeleton, nascent hydrogen reduction yields N-monodesmethyl thalicarpine which is methylated.

Abstract: There is provided a novel simaroubolide derived from Brucea antidysenterica which possesses high and surprising anti-leukemic activity at dosage levels of micrograms per kilogram body weight.