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Wang, Li-Ying,Wang, Xiu-Hua,Tan, Jia-Lian,Xia, Shuai,Sun, Heng-Zhi,Shi, Jin-Wen,Jiang, Ming-Dong,Fang, Liang,Zuo, Hua,Dupati, Gautam,Jang, Kiwan,Shin, Dong-Soo Korean Chemical Society 2012 Bulletin of the Korean Chemical Society Vol.33 No.11
A number of novel small molecules, safrole oxide derivatives 4a-c, 6a-c, 9a-h, were synthesized by the reaction of safrole oxide with anilines 3 and 5, or its alkyl allyl ether derivative 7 with alkyl bromide 8 in moderate yields. The antiproliferative effects of all the target molecules on A549 cell growth were investigated and it was found that the 14 novel compounds could suppress A549 lung cancer cell growth. Among them, compound 6b was the most effective compound in inhibiting the proliferation of A549 cells.
Yi Xiang,Xiu-Hua Wang,Quan Yang,Jia-Lian Tan,장희재,Hua Zuo,신동수 대한화학회 2018 Bulletin of the Korean Chemical Society Vol.39 No.2
Inappropriate thrombus formation within blood vessels is the leading cause of mortality in the industrialized world. Platelet aggregation activated by thrombin may have close relationship with thrombosis. Based on our studies on the pharmacophoric role of 1,4-benzoxazine-3(4H)-one for desirable platelet aggregation inhibitory activity, we identified N-(4-ethyl-3-oxo-3,4-dihydro-2H-benzo[b][1,4]oxazin-7-yl)-2-(4-methylpiperazin-1-yl)acetamide (BOAP-AM6) and N-(4-butyl-3-oxo-3,4-dihydro-2H-benzo[b][1,4]oxazin-7-yl)-2-(4-(4-fluorophenyl)piperazin-1-yl)acetamide (BOAP-AM21) as platelet aggregation inhibitors with an IC50 of 8.93 and 8.67 μM, respectively, as potent as the positive control aspirin. A combination of structure–activity relationships studies and molecular modeling revealed that the molecule BOAP-AM6 interacted with the amino acid residue TYR166 and ARG214 in the binding site of GPIIb/IIIa receptor through hydrogen bond and compound BOAP-AM21 acted on the amino acid residue ASN215 and ALA218, both through the same approach as the reported potent molecules 7a and 7b.
Li-Ying Wang,Xiu-Hua Wang,Jia-Lian Tan,Shuai Xia,Heng-Zhi Sun,Jin-Wen Shi,Ming-Dong Jiang,Liang Fang,Hua Zuo,Gautam Dupati,장기완,신동수 대한화학회 2012 Bulletin of the Korean Chemical Society Vol.33 No.11
A number of novel small molecules, safrole oxide derivatives 4a-c, 6a-c, 9a-h, were synthesized by the reaction of safrole oxide with anilines 3 and 5, or its alkyl allyl ether derivative 7 with alkyl bromide 8 in moderate yields. The antiproliferative effects of all the target molecules on A549 cell growth were investigated and it was found that the 14 novel compounds could suppress A549 lung cancer cell growth. Among them, compound 6b was the most effective compound in inhibiting the proliferation of A549 cells.
Synthesis of N-Azaaryl Anilines: An Efficient Protocol via Smiles Rearrangement
Xia, Shuai,Wang, Li-Ying,Sun, Heng-Zhi,Yue, Huan,Wang, Xiu-Hua,Tan, Jia-Lian,Wang, Yin,Hou, Di,He, Xiao-Yan,Mun, Ki-Cheol,Kumar, B. Prem,Zuo, Hua,Shin, Dong-Soo Korean Chemical Society 2013 Bulletin of the Korean Chemical Society Vol.34 No.2
An efficient process for the synthesis of N-azaaryl anilines via Smiles rearrangement as a tool. A variety of N-azaaryl anilines were generated by the reaction of substituted phenols, substituted anilines, aminopyridines and chloroacetyl chloride or pyridols, under base condition in good to excellent yields.
Synthesis of N-Azaaryl Anilines: An Efficient Protocol via Smiles Rearrangement
Shuai Xia,Li-Ying Wang,Heng-Zhi Sun,Huan Yue,Xiu-Hua Wang,Jia-Lian Tan,Yin Wang,Di Hou,Xiao-Yan He,Ki-Cheol Mun,B. Prem kumar,Hua Zuo,신동수 대한화학회 2013 Bulletin of the Korean Chemical Society Vol.34 No.2
An efficient process for the synthesis of N-azaaryl anilines via Smiles rearrangement as a tool. A variety of Nazaaryl anilines were generated by the reaction of substituted phenols, substituted anilines, aminopyridines and chloroacetyl chloride or pyridols, under base condition in good to excellent yields.