Preparation of phenyltriazoles and related compounds as antitumor agents.

Abstract

Title compds. I [R4 = (R4')n; n = 0-3; R3, R4' = H, halo, CN, etc.; Q = 5-membered heteroaryl ring with provisos; L = CONH, NHCO, C(S)NH, etc.; R2 = 5 to 12-membered heteroaryl with provisos] and their pharmaceutically acceptable salts and formulations were prepd. For example, Na(AcO)3BH/isobutyraldehyde mediated reductive amination of amine II [X = H] afforded phenyltriazole II [X = CH2CH(CH3)2]. In B-raf kinase inhibition assays, compds. I exhibited IC50 values less than 100 nM. [on SciFinder(R)]