In 2022,Shen, Dadong; Liu, Hanyu; Qian, Feng; Wang, Pu published an article in Bioorganic Chemistry. The title of the article was 《Design, synthesis and evaluation of novel thienopyridazine derivatives as Chk1/2 inhibitors》.Related Products of 768-35-4 The author mentioned the following in the article:
In order to search for novel checkpoint kinase 1/2 (Chk1) inhibitors, a series of new compounds I.HCl [X = H2C, HN; R = 4-MeO, 4-Cl, 3-Cl, etc.; R1 = pyrrolidin-3-ylmethyl, 3-piperidylmethyl, 3-piperidyl, (3S)-3-piperidyl, 4-piperidyl; R2 = H, Me, Et, etc.] and II [X = H2C, HN; R = 4-MeO, 4-Cl, 3-Cl, etc.; R2 = H, Me, Et, etc.; R3 = (1-tert-butoxycarbonylpyrrolidin-3-yl)methyl, (1-tert-butoxycarbonyl-3-piperidyl)methyl, 1-tert-butoxycarbonylazetidin-3-yl, etc.] incorporating thienopyridazine core were designed and synthesized. Bioevaluation showed that compounds I.HCl [X = HN, R = 3-Cl, R1 = 3-piperidylmethyl, R2 = Et; X = HN, R = 2-Cl, R1 = pyrrolidin-3-ylmethyl, R2 = Et; X = H2C, R = 4-Cl, R1 = 3-piperidyl, R2 = Me; X = HN, R = 3-F, R1 = (3S)-3-piperidyl, R2 = H] exhibited relatively good inhibitory activity. Notably, compound I.HCl [X = HN, R = 3-F, R1 = (3S)-3-piperidyl, R2 = H] displayed high selectivity against a panel of kinases and inhibited Chk1/2 signaling pathway stimulated by DNA damage drugs in cellular level. Mol. docking of I.HCl [X = HN, R = 3-F, R1 = (3S)-3-piperidyl, R2 = H] to the ATP-binding site of Chk1 kinase domain indicated the existence of polar interactions between I.HCl [X = HN, R = 3-F, R1 = (3S)-3-piperidyl, R2 = H] and the ATP-ribose-binding residues of Chk1. In mouse HT-29 xenografts, a synergistic effect was observed Co-treatment by CPT-11 and I.HCl [X = HN, R = 3-F, R1 = (3S)-3-piperidyl, R2 = H] significantly diminished the tumor volume, indicating the great potential of I.HCl [X = HN, R = 3-F, R1 = (3S)-3-piperidyl, R2 = H] as a candidate of Chk1/2 inhibitor. In the experiment, the researchers used (3-Fluorophenyl)boronic acid(cas: 768-35-4Related Products of 768-35-4)
(3-Fluorophenyl)boronic acid(cas: 768-35-4) can be used to make novel liquid crystalline fluorobiphenylcyclohexenes and difluoroterphenyls by palladium-catalyzed cross-couplings also used in the synthesis of o-phenylphenols as potent leukotriene B4 receptor agonists.Related Products of 768-35-4
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics