Synthesis and in vitro antimetabolic evaluation of some steroidal thiazoles
1989 ◽
Vol 54
(12)
◽
pp. 3339-3347
◽
Keyword(s):
Steroidal thiazoles VI-XII have been synthesized. The starting bromoketones XVII and XX were prepared by bromination of pregnan-20-ones in position 21 with copper(II) bromide, and used for synthesis of the thiazole derivatives employing the Hantzch reaction. Preliminary biological evaluation of thiazoles I-XII against the P388 lymphocytic leukemia cell line showed growth inhibition values of ED50 2.9 and 7 μg/ml for thiazoles II and VII, respectively.