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문형룡,Ah-Young Park,Kyung Ran Kim,Hyung-Rock Lee,Jin-Ah Kang,Won Hee Kim,천부순,Pervez Ahmad,정낙신 대한화학회 2008 Bulletin of the Korean Chemical Society Vol.29 No.12
5''-Iodoneplanocin A (1) and its analogues 2 and 3 were designed and synthesized as potential SAHH inhibitor via iodocyclopentenol 6, which was prepared using a Michael addition-iodination-elimination process. All final compounds did not show antiviral activity, maybe due to a steric hindrance induced by 5''-iodo substituent.
Synthesis of Methyl-substituted Bicyclic Carbanucleoside Analogs as Potential Antiherpetic Agents
문형룡,Kyung Ran Kim,Ah-Young Park,Hyung-Rock Lee,Jin-Ah Kang,Won Hee Kim,천부순,Jang Ho Bae,정낙신 대한화학회 2008 Bulletin of the Korean Chemical Society Vol.29 No.10
Novel bicyclo[3.1.0]hexanyl purine nucleoside analogues were synthesized as potential antiherpetic agents via a bicyclo[3.1.0]hexanol (±)-8, which was prepared using a highly efficient carbenoid cycloaddition reaction. A highly diastereoselective reduction of ketone and a Mitsunobu reaction for the condensation of glycosyl donor (±)-12 with 6-chloropurine were employed.
Acyclonucleoside 류의 합성(3) -Ribavirin 유도체의 합성-
문형룡(Hyung Ryong Moon),양재욱(Jae Wook Yang),김문환(Moon Hwan Kim),천문우(Moon Woo Chun),정원근(Won Keun Chung) 대한약학회 1989 약학회지 Vol.33 No.6
The Synthesis of acyclic derivatives of ribavirin (2''-azido and halo seco derivatives) for the development of new antiviral agents is described. These acyclic nucleosides are synthesized from ribavirin by the method of ring opening reaction of sugar moietry.
김정수,천부순,문형룡 대한화학회 2013 Bulletin of the Korean Chemical Society Vol.34 No.5
Based on the finding that the 2-aminobenzamido group of MS-275 plays a crucial role in inhibiting HDACs through chelation of zinc existing at the active site of HDAC enzymes, novel N-(2-hydroxyphenyl)arylsulfonamide derivatives were synthesized for their potential ability to inhibit HDACs and evaluated for anticancer activity against human breast cancer cell line (MCF-7). Although the synthesized arylsulfonamides have failed to significantly inhibit total HDACs activity, phenyl carbamate-linked arylsulfonamide 10 and benzyl thiocarbamate-linked arylsulfonamide 15 exhibited good anticancer activities, which were only 4.3- and 3.6-fold lower anticancer activities, respectively, than MS-275 that is undergoing phase II clinical trials. These results suggest that these compounds may act as a selective HDAC inhibitor and probably N-(2-hydroxyphenyl) sulfamoyl group may play an important role in interacting with HDAC enzymes through chelation of zinc ion.
새로운 사이클로프로필 뉴크레오사이드 유도체의 합성과 생리활성
강진아(Jin-Ah Kang),천부순(Pusoon Chun),문형룡(Hyung Ryong Moon) 대한약학회 2012 약학회지 Vol.56 No.4
Synthesis of novel cyclopropyl pyrimidine and purine nucleoside derivatives 2~8 with α-configuration was successfully accomplished using an epoxide-ring opening reaction, lactonization, a hydroboration-oxidation reaction and a Mitsunobu reaction as the key steps. Antiviral activities against HSV-1 and -2, HIV-1 and -2, coxsackie B1and B3 viruses and poliovirus were assayed. Three compounds 4, 7 and 8 exhibit cytotoxicity-derived antiviral activity only in HIV-1 and -2.
박민희,김성진,정해영,문경미,손수진,김대현,김혜림,김민조,문형룡,Pusoon Chun,제남경,Takako Yokozawa,정형오,윤휘영 대한약학회 2015 Archives of Pharmacal Research Vol.38 No.4
Tyrosinase inhibitors might have potential usein cosmetic and medicinal products for the prevention ofpigmentation disorders. However, only a few inhibitors arecurrently used due to their cytotoxicity, and lack ofselectivity and stability. In this study, we synthesizedseveral tyrosinase inhibitors and investigated their activity. To investigate the action of 2-[4-(5-chlorobenzo[d]thiazol-2-yl)phenoxy]-2-methylpropanoic acid (MHY908) specificallyin the inhibition of melanogenesis, a mushroomtyrosinase activity assay was performed. We confirmed theinhibitory effect of MHY908 at various melanin concentrationsusing a-MSH-induced melanoma cells. Our resultsindicate that MHY908 potently inhibited mushroomtyrosinase activity (IC50 = 8.19 lM) in a dose-dependentmanner. Through a docking simulation, we also analyzedits binding mode to inhibit tyrosinase activity. MHY908also decreased melanin synthesis without inducing cytotoxicity. These results suggest that MHY908 is a goodcandidate for prevention and treatment of pigmentationdisorders.
Seong Jin Kim,Youngwoo Woo,Ah-Young Park,김혜림,손수진,윤휘영,천부순,문형룡 대한화학회 2014 Bulletin of the Korean Chemical Society Vol.35 No.9
Synthesis of north-5′-methylbicyclo[3.1.0]hexyl adenine and hypoxanthine nucleosides with an ethenyl group at C3′ position was successfully achieved by a highly facile method. Methylbicyclo[3.1.0]hexanone (±)-7 with three contiguous chiral centers and its epimer (±)-6 was remarkably simply constructed only by four steps involving a carbenoid insertion reaction in the presence of rhodium (II) acetate dimer as a metal catalyst, giving a correct relative stereochemistry of the generated three chiral centers. Due to steric hindrance from the concave face of the bicyclo[3.1.0]hexanone system, a Grignard reaction of (±)-7 with ethenylmagnesium bromide showed exclusive diastereoselectivity towards the b-face. The Grignard reaction chemoselectively proceeded without reacting with ester functionality. Coupling reaction of glycosyl donor (±)-11 with 6-chloropurine nucleobase afforded only the desired N9-alkylated nucleoside without the formation of N7-regioisomer. By the conventional method, 6-chloro group was converted into 6-amino and 6-hydroxy groups to give the desired adenine and hypoxanthine bicyclo[3.1.0]hexyl carbanucleosides with 3′-ethenyl group, respectively.
벤조[b][1,4]옥사진-3(4H)-치온 유도체의 합성과 이들의 타이로시네이즈 저해 활성
김도현(Do Hyun Kim),천부순(Pu soon Chun),정해영(Hae Young Chung),문형룡(Hyung Ryong Moon) 대한약학회 2017 약학회지 Vol.61 No.1
To investigate whether a “β-phenyl-α,β-unsaturated thiocarbonyl” scaffold can play a key role in tyrosinase inhibition, benzo[b][1,4]oxazine-3(4H)-thione derivatives bearing the scaffold were synthesized through a three-step reaction including Knoevenagel condensation. Four compounds showed not only high binding affinity with tyrosinase on docking simulation but also greater inhibitory activity against mushroom tyrosinase than arbutin. These results indicate that a “β- phenyl-α,β-unsaturated thiocarbonyl” may serve as an important chemical scaffold for potent tyrosinase inhibitors.
So Hee Kim,하영미,Kyoung Mi Moon,최연자,박윤정,Hyoung Oh Jeong,정기웅,Hye Jin Lee,천부순,문형룡,정해영 대한약학회 2013 Archives of Pharmacal Research Vol.36 No.10
We synthesized (Z)-5-(2,4-dihydroxybenzylidene)thiazolidine-2,4-dione (MHY498) as a potential tyrosinaseinhibitor. MHY498 potently inhibited mushroomtyrosinase activity (mean IC50 = 3.55 lM) in a dosedependentmanner.MHY498 was more potent than the wellknowntyrosinase inhibitor, kojic acid (mean IC50 = 22.79lM). When tested in B16F10 melanoma cells treated witha-melanocyte stimulating hormone (a-MSH), MHY498inhibited murine tyrosinase activity and decreased melaninproduction without inducing cytotoxicity. Docking modelsshowed that the binding affinity of MHY498 to tyrosinasewas higher than that of kojic acid, and docking simulationresults indicated that the tyrosinase binding moieties ofMHY498 and kojic acid were similar. Western blottingshowed that tyrosinase inhibition by MHY498 partly resultedfrom the expressional modulations of tyrosinase and itstranscription factor, microphthalmia-associated transcriptionfactor, via the cAMP–PKA–CREB pathway. Thesefindings suggest that MHY498 could be useful as an antimelanogenicagent for the prevention and treatment of diseasesassociated with skin pigmentation.