6E-hydroximinosteroid homodimerization by cross-metathesis processes.
A rapid and efficient synthesis of 6E-hydroximinosteroid homodimers is described. The two new compounds were linked at position 3 of the steroid nucleus via a ruthenium catalyzed cross-metathesis reaction. The cytotoxic activity of these compounds was evaluated in vitro on human lung carcinoma A549 (ATCC CCL-185), colon adenocarcinoma HCT-116 (ATCC CCL-247), human caucasian glioblastoma multiforme T98G (ECACC 92090213) and human pancreatic adenocarcinoma PSN1 (ECACC 94060601) tumour cells. Homodimer 10b presented selective activity against HCT-116, although they are not highly toxic when compared with the monomer counterparts.
Rega
Miriam
M
Departamento de Química Fundamental, Facultad de Ciencias, Universidad de A Coruña, A Coruña, Spain.
Jiménez
Carlos
C
Rodríguez
Jaime
J
D016923:Cell Death / Q000187:drug effects; D045744:Cell Line, Tumor; D002625:Chemistry, Organic / Q000379:methods*; D019281:Dimerization; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D020128:Inhibitory Concentration 50; D013256:Steroids / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
C525525:6E-hydroximinosteroid; D013256:Steroids