Synthesis and structure-activity relationship study of triazine-based inhibitors of the DNA binding of NF-κB was written by Fujii, Shinya;Kobayashi, Takanobu;Nakatsu, Aki;Miyazawa, Hiroshi;Kagechika, Hiroyuki. And the article was included in Chemical & Pharmaceutical Bulletin in 2014.Category: chlorides-buliding-blocks The following contents are mentioned in the article:
Nuclear transcription factor nuclear factor-κ B (NF-κB) has diverse pathophysiol. functions, and NF-κB inhibitors are considered to be candidates for multiple therapeutic applications. The previously reported novel triazine-based NF-κB inhibitor, 2-anilino-4,6-dichloro-1,3,5-triazine (NI241), directly inhibits DNA binding of NF-κB. Here, the synthesis of a series of triazine derivatives I (R1 = Cl, BuO, NHMe, NMe2; R2 = MeO, OC6H5, N-pyrrolidino, etc.) II (R3 = H, Me, Et, etc.; R4 = C6H5, 2-MeOC6H4, 3-MeOC6H4, etc.) and evaluation of their structure-activity relationships for NF-κB inhibition are reported. The 2-amino-4,6-dichloro-1,3,5-triazine substructure is essential for the inhibitory activity of the lead compound NI241, and modification of NI241 by introduction of an m-methoxy substituent on the Ph ring afforded the more potent derivative The structure-activity relationships identified in this study suggested a possible mechanism of irreversible NF-κB inhibition by NI241, and should be helpful in the design of other NF-κB inhibitors. This study involved multiple reactions and reactants, such as 4,6-Dichloro-N-phenyl-1,3,5-triazin-2-amine (cas: 2272-40-4Category: chlorides-buliding-blocks).
4,6-Dichloro-N-phenyl-1,3,5-triazin-2-amine (cas: 2272-40-4) belongs to organic chlorides. Organochlorines stimulate the central nervous system and cause convulsions, tremor, nausea, and mental confusion. Examples are dichlorodiphenyltrichloroethane (DDT), chlordane, lindane, endosulfan, and dieldrin. Aliphatic organochlorides are often alkylating agents as chlorine can act as a leaving group, which can result in cellular damage.Category: chlorides-buliding-blocks
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics