In 2017,Arai, Midori A.; Utsumi, Takao; Yanase, Natsuki; Fujimatsu, Teruhisa; Ishibashi, Masami published 《Efficient synthesis of heterocyclic flavonoids with hedgehog signal inhibitory activity》.Chemical & Pharmaceutical Bulletin published the findings.Safety of 2-Bromonicotinaldehyde The information in the text is summarized as follows:
A series of heterocyclic flavonoids I [R = 5-Br, 6-Br, 2-Br; R1 = H, 4-Me, 2-Br-4,5-(OCH3)2, 2-Br, etc.; X = OCH2OCH3, OH, OCH2OSi(CH3)2C(CH3)3] was evaluated for their Hh signaling inhibitory activity on cancer cell lines using our cell-based assay system. Among the synthetic flavonoids, compounds I (R = 5-Br, 2-Br; R1 = 2-Br; X = OCH2OCH3) showed good inhibitory activity (IC50 was 16.8 and 21.8 μM, resp.), and were cytotoxic toward human pancreatic (PANC1) and prostate (DU145) cancer cells in which Hh signaling was activated. Compounds I (R = 5-Br, 2-Br; R1 = 2-Br; X = OCH2OCH3) had moderate selectivity against PANC1 cells. Western blotting analyses revealed that PTCH and GLI1 expression was reduced after treatment with these compounds Overall, these synthetic flavonoids represent promising new additions to this expanding panel of Hh pathway inhibitors, and with further development these mols. may ultimately be considered for clin. use. In the experiment, the researchers used many compounds, for example, 2-Bromonicotinaldehyde(cas: 128071-75-0Safety of 2-Bromonicotinaldehyde)
2-Bromonicotinaldehyde(cas: 128071-75-0) belongs to pyridine. Pyridine is very deactivated towards electrophilic substitution with respect to benzene. For this reason classical formylation, using methods such as the Gattermann or Vilsmeier reactions, are not generally successful. Safety of 2-Bromonicotinaldehyde