Discovery of a Novel 2,6-Difunctionalized 2H-Senzopyran Inhibitors Toward Sphingosylphosphorylcholine Synthetic Pathway as New Anti-inflammatory Target

作者：Lee Gee Hyung; Lee Seong Jin; Jeong Dae Young; Kim Ha Young; Lee Doohyun; Lee Taeho; Hwang Jong Yeon; Park Woo Kyu; Kong Jae Yang; Cho Heeyeong^*; Gong Young Dae

来源：BULLETIN OF THE KOREAN CHEMICAL SOCIETY, 2014, 35(8): 2385-2390.

DOI：10.5012/bkcs.2014.35.8.2385

• Sphingosylphosphorylcholine
• Anti-inflammatory inhibitors
• Drug-like library
• 2H-benzopyran
• Small molecules

Novel 2,6-difuctionalized 2H-benzopyrans were synthesized and evaluated for a sphingosylphosphorylcholine (SPC) inhibitor. The synthetic 2H-benzopyrans 1c and 3a showed high potency in SPC-induced cell proliferation assay (IC50 %26lt; 20 nM). Neither hERG K+ channel binding (%26gt; 10 mu M) nor CYP inhibitions (%26gt; 10 mu M) were observed. Also, the simple structure-activity relationship (SAR) results were obtained from analysis of 2H-benzopyran derivatives 1-3 and the anti-SPC effect of 2H-benzopyran 1c was confirmed by a HUVEC tube formation assay.

• 出版日期2014-8-20