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3‐Cyano‐4,6‐disubstituted‐2(1 H )‐imino or oxopyridines: New Antineoplastic Agents with High Selectivity Towards Leukemia Cell Lines
Author(s) -
Abadi A. H.,
AlKhamees H. A.
Publication year - 1998
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/(sici)1521-4184(199810)331:10<319::aid-ardp319>3.0.co;2-v
Subject(s) - leukemia , substituent , selectivity , chemistry , growth inhibition , cell culture , stereochemistry , cell growth , biochemistry , immunology , biology , genetics , catalysis
Two series of 3‐cyano‐2(1 H )‐oxopyridine and 3‐cyano‐2(1 H )‐iminopyridine derivatives carrying various aryl substituents at position 4 and (4‐((7‐chloro or trifluoromethylquinol‐4‐yl)amino)phenyl) substituent at position 6 were synthesized and evaluated for their antitumor activity. Compounds 3f and 6d showed high selectivity towards leukemia cell lines with full panel median growth inhibition GI 50 average sensitivity towards all cell lines (MG‐MID) at 7.9 and 19.7 μM and leukemia subpanel GI 50 average sensitivity towards leukemia cell lines (MG‐MID) at 1.74 and 2.9 μM, respectively, also they exhibited full panel total growth inhibition TGI (MG‐MID) at 34.8 and 59.0 μM and leukemia subpanel TGI (MG‐MID) at 5.3 and 13.5 μM, respectively.