Brusatolyl esters

A series of new bisbrusatolyl and brusatolyl esters and related compounds were synthesized and tested for in vivo antileukemic activity against a quassinoid sensitive strain of P-388 lymphocytic leukemia in BDFi mice as shown in Table 8. Bisbrusatolylmalonate (81), bisbrusatolylsuccinate (82), bisbrusatolylglutarate (83), bisbrusatolyladipate (84), and bisbrusatolyl sebacate (85) were as active as, or more active than, brusatol (8). The C-3 esters of brusatol (8) or bruceantin (1) were also as active as, or more active than, the original brusatol (8) and bruceantin (1) in general. 

Free hydroxy groups at C-11 and C-12, as well as the enone double bond in ring-A of both bisbrusatolyl and brusatolyl esters, are required for antileuJcemic activity. The presence of a double bond in the ester side chain contributes slightly to the enhanced activity of these esters [30]. 

Table 8. Anti leukemic Activity of Bisbrusatolyl and Brusatolyl Esters and Related Compounds against P>388 Lymphocytic Leukemia Cell Growth in BDFl Mice...

A series of bis-(brusatolyl) esters (55b) has been synthetized and tested for in vivo antileukemic activity. The bis-(brusatolyl) malonate, succinate, glutarate, adipate and sebacate were as active or more active than brusatol (55a) 51). 

Lee, K. H., M. Okano, I. H. Hall, D. A. Brent, and B. Soltmann Antitumor Agents XLV Bisbrusatolyl and Brusatolyl Esters and Related Compounds as Novel Potent Antileukemic Agents. J. Pharm. Sci. 71, 338 (1982). 

---

See also in sourсe #XX -- [ , , ]

See also in sourсe #XX -- [ , , ]

---