Quinolinium salt as a potent inhibitor of lymphocyte apoptosis.
The synthesis of several quinolinium salts and related compounds and their ability to inhibit glucocorticoid-induced apoptosis in murine thymocytes are described. Interestingly, 1-[2-methoxyimino-2-(4-pyrrolidin-1-yl-phenyl)ethyl]quinolinium bromide (11) showed a potent protective effect with an EC(50) of 0.013 microM, which was at least 300-fold more potent than the reference compound pifithrin-alpha.
Barchéchath
Sylvie D
SD
Department of Chemistry and Biochemistry, University of California, San Diego, La Jolla, CA 92093-0663, USA.
Tawatao
Rommel I
RI
Corr
Maripat
M
Carson
Dennis A
DA
Cottam
Howard B
HB
D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D017209:Apoptosis / Q000187:drug effects*; D052160:Benzothiazoles; D005938:Glucocorticoids / Q000494:pharmacology; D006801:Humans; D008214:Lymphocytes / Q000166:cytology / Q000187:drug effects*; D011806:Quinolinium Compounds / Q000138:chemical synthesis* / Q000494:pharmacology; D012492:Salts / Q000737:chemistry*; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000494:pharmacology; D014050:Toluene / Q000031:analogs & derivatives* / Q000494:pharmacology; D014407:Tumor Cells, Cultured
D000970:Antineoplastic Agents; D052160:Benzothiazoles; D005938:Glucocorticoids; D011806:Quinolinium Compounds; D012492:Salts; D013844:Thiazoles; D014050:Toluene; C018435:quinolinium dibromide; C121565:pifithrin