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Synthesis and Biological Evaluation of 2-Aminoisonicotinic Acid Analogues as HIF-1α Inhibitors. -A series of 2-aminoisonicotinic acid derivatives such as (I) and (II) is synthesized and evaluated for their in vitro HIF-1 inhibitory activity. Especially, compound (Id) shows good inhibitory properties. -(XIA, Y.; WON, M.; KANG, J. E.; PARK, S.-K.; LEE, K.; KIM, H.-M.; LEE*, K.; Bull. Korean Chem. Soc. 31 (2010) 12, 3828-3829, http://dx.doi.org/10.5012/bkcs.2010.31.12.3826 ; Coll. Pharm., Dongguk Univ., Seoul 100-715, S. Korea; Eng.) -R. Langenstrassen 15-153