53391-78-9Relevant academic research and scientific papers
Synthesis of Fluorescent Probes Targeting Tumor-Suppressor Protein FHIT and Identification of Apoptosis-Inducing FHIT Inhibitors
Kawaguchi, Mitsuyasu,Sekimoto, Eriko,Ohta, Yuhei,Ieda, Naoya,Murakami, Takashi,Nakagawa, Hidehiko
supporting information, p. 9567 - 9576 (2021/07/19)
For the early diagnosis of cancer, leading to a better chance of full recovery, marker genes whose expression is already altered in precancerous lesions are desirable, and the tumor-suppressor gene FHIT is one candidate. The gene product, FHIT protein, has a unique dinucleoside triphosphate hydrolase (AP3Aase) activity, and in this study, we designed and synthesized a series of FHIT fluorescent probes utilizing this activity. We optimized the probe structure for high and specific reactivity with FHIT and applied the optimized probe in a screening assay for FHIT inhibitors. Screening of a compound library with this assay identified several hits. Structural development of a hit compound afforded potent FHIT inhibitors. These inhibitors induce apoptosis in FHIT-expressing cancers via caspase activation. Our results support the idea that FHIT binders, no matter whether inhibitors or agonists of AP3Aase activity, might be promising anticancer agents.
Modified coumarins. 7. Synthesis and biological activity of mannich bases of substituted 7,8,9,10-tetrahydrobenzo[c]chromen-6-ones
Garazd,Panteleimonova,Garazd,Khilya
, p. 532 - 538 (2007/10/03)
Condensation of 1- and 3-hydroxy-7,8,9,10-tetrahydrobenzo[c]chromen-6-ones with substituted 1,1-diaminomethanes produced Mannich bases containing a dialkylaminomethyl group in the 2- and 4-positions of 7, 8,9,10-tetrahydrobenzo[c]chromen-6-one. Pharmacological screening of 2-chloro-3-hydroxy-4-(1-pyrrolidinylmethyl)-7,8,9,10-tetrahydro-6H-benzo[c] chromen-6-one in Wistar rats showed that it possesses low toxicity and acts as a stimulant of the central and peripheral nervous systems with indications of neuroleptic and tranquilizing activities.
