1418005-85-2Relevant academic research and scientific papers
Dual structure-activity relationship of osteoclastogenesis inhibitor methyl gerfelin based on teg scanning
Kanoh, Naoki,Suzuki, Takahiro,Kawatani, Makoto,Katou, Yasuhiro,Osada, Hiroyuki,Iwabuchi, Yoshiharu
, p. 44 - 52 (2013)
Methyl gerfelin derivatives, each having an amine-terminated tri(ethylene glycol) linker at the peripheral position, were designed and systematically synthesized. These TEGylated derivatives were then subjected to a structure-activity relationship (SAR) study to examine their glyoxalase 1-inhibition activity and binding affinity toward the three binding proteins identified. Among the derivatives synthesized, that with a NH2-TEG linker at the C6-methyl group showed the most potent glyoxalase 1-inhibiting activity and glyoxalase 1 selectivity. These results indicated that derivatization at the C6-methyl group would be suitable for the further development of selective glyoxalase 1 inhibitors.
