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Sharma, Vinay K.,Lee, Ki-Cheul,Joo, Cheon-Ik,Sharma, Niti,Jung, Sang-Hun Korean Chemical Society 2011 Bulletin of the Korean Chemical Society Vol.32 No.suppl8
To investigate the possible isosteric replacement of imidazolidinone moiety in 4-phenyl-N-arylsulfonylimidazolidinone for broad and potent anticancer agents, a series of 4-phenyl-l(N)-arylsulfonylimidazolidinones 6a-k, imidazolidinethione analogs 7a-i, and imidazolidine oxime analogs 8a-c were prepared and evaluated for their in vitro anticancer activity against four human cancer cell lines (human lung A549, human colon COLO205, human leukemia K562, human ovary SK-OV-3). Among all the derivatives of N-arylsulfonylimidazolidinone 6a-k, compounds 6f and 6g showed the best inhibition comparable to doxorubicin against all cancer cell lines. Increasing the carbon chain on alkyl moieties of carbamates as shown in 6c-g did not alter the activity. The imidazolidinethione analogs 7a-i and imidazolidin-2-one oxime derivatives 8a-c did not possess any good activity. Therefore, imidazolidinone moiety is the best pharmacophore among the 4-phenyl-Narylsulfonylimidazolidinone derivatives.
Vinay K. Sharma,이기철,Cheonik Joo,Niti Sharma,정상헌 대한화학회 2011 Bulletin of the Korean Chemical Society Vol.32 No.8
To investigate the possible isosteric replacement of imidazolidinone moiety in 4-phenyl-N-arylsulfonylimidazolidinone for broad and potent anticancer agents, a series of 4-phenyl-l(N)-arylsulfonylimidazolidinones 6ak,imidazolidinethione analogs 7a-i, and imidazolidine oxime analogs 8a-c were prepared and evaluated for their in vitro anticancer activity against four human cancer cell lines (human lung A549, human colon COLO205, human leukemia K562, human ovary SK-OV-3). Among all the derivatives of N-arylsulfonylimidazolidinone 6a-k, compounds 6f and 6g showed the best inhibition comparable to doxorubicin against all cancer cell lines. Increasing the carbon chain on alkyl moieties of carbamates as shown in 6c-g did not alter the activity. The imidazolidinethione analogs 7a-i and imidazolidin-2-one oxime derivatives 8a-c did not possess any good activity. Therefore, imidazolidinone moiety is the best pharmacophore among the 4-phenyl-Narylsulfonylimidazolidinone derivatives.
Bile duct injury during laparoscopic cholecystectomy: An Indian e-survey
Supriya Sharma,Anu Behari,Ratnakar Shukla,Mukteshwar Dasari,Vinay K. Kapoor 한국간담췌외과학회 2020 Annals of hepato-biliary-pancreatic surgery Vol.24 No.4
Backgrounds/Aims: In the absence of national registry of laparoscopic cholecystectomy (LC) or its complications, it is impossible to determine incidence of bile duct injury (BDI) in India. We conducted an e-survey among practicing surgeons to determine prevalence and management patterns of BDI in India. Our hypothesis was that majority of surgeons would have experienced a BDI during LC despite large experience and that most surgeons who have a BDI tend to manage it themselves. Methods: An 18-question e-survey of practicing laparoscopic surgeons in India was done. Results: 278/727 (38%) surgeons responded. 240/278 (86%) respondents admitted to a BDI during LC and 179/230 (78%) affirmed to more than one BDI. A total of 728 BDIs were reported. 36/230 (15%) respondents experienced their first BDI even after >10 years of practice and 40% had their first BDI even after having performed >100 LCs. 161/201 (80%) of the respondents decided to manage the BDI themselves, including 56/99 (57%) non-biliary surgeons and 44/82 (54%) surgeons working in non-biliary center. 37/201 (18%) respondents admitted to having a mortality arising out of a BDI; the mortality rate of BDI was 37/728 (5%) in this survey. Only 13/201 (6%) respondents have experienced a medico-legal case related to a BDI during LC. Conclusions: Prevalence of BDI is high in India and occurs despite adequate experience and volume. Even inexperienced non-biliary surgeons working in non-biliary centers attempt to repair the BDI themselves. BDI is associated with significant mortality but litigation rates are fortunately low in India.
Synthesis of Water Soluble Analogs of Arylsulfonylimidazolidinone (JSH-2282)
방성철,이기철,Vinay K. Sharma,Niti Sharma,Hyun-Sun Yang,정상헌 대한화학회 2013 Bulletin of the Korean Chemical Society Vol.34 No.7
To improve the water solubility of arylsulfonylimidazolidinone (JSH-2282), a potent anti-cancer agent, two urea derivatives, sodium (S)-2-(3-(4-(5-((S)-2-oxo-4-phenylimidazolidin-1-ylsulfonyl)indoline-1-carbonyl)- phenyl)ureido)succinate (2a) and sodium (S)-2-(3-(4-(5-((S)-2-oxo-4-phenylimidazolidin-1-ylsulfonyl)indoline- 1-carbonyl)phenyl)ureido)pentanedioate (2b), were synthesized and studied for solubility and anti-cancer activity.
Study on IL-5 Inhibitory Activity of Novel Chromenone Derivatives
Eeda Venkateswararao,Vinay K. Sharma,Ki-Cheul Lee,Eunmiri Roh,Youngsoo Kim,Sang-Hun Jung 충남대학교 약학대학 의약품개발연구소 2013 藥學論文集 Vol.28 No.-
A novel series of chromenone analogs were synthesized and evaluated for their inhibitory activity against interleukin-5. Among them compounds 5-(cyclohexylmethoxy)-N-(4-hydroxy-3-(hydroxymethyl)phenyl)-4-oxo-4H-chromene-3-carboxamide (8e, 54% inhibition at 30 μM) and ethyl 3-(5-(cyclohexylmethoxy)- 4-oxo-4H-chromene-3-carboxamido)benzoate (8g, 62% inhibition at 30 μM) showed the most potent activity. The SAR activity of these chromenones indicated that the bulky substituents at ring B increases the inhibition against IL-5 though none of the compound showed potent inhibition. The reason for less activity of the chromenones 8a-h may be due to the rigidity of amine linkage.
Santhosh Subramanian,Vinay K. Sharma,Jieun Yun,정상헌 대한화학회 2014 Bulletin of the Korean Chemical Society Vol.35 No.10
To investigate the possible isosteric replacement of imidazolidinone moiety in 4-phenyl-1-arylsulfonylimidazolidinones (2) for broad and potent anti-cancer agents, a series of 5-phenyl-1H-pyrazol-3-yl 1- (acyl)indoline-5-sulfonates (4) and 1-(1-(acyl)indolin-5-ylsulfonyl)-5-phenylpyrazolidin-3-ones (5) were prepared and evaluated for their cytotoxicity against six human cancer cell lines. Although the pyrazoles 4 or pyrazolidinones 5 showed relatively good activity, still they showed lesser activity in comparison to imidazolidinones 2. These activity decreases could be interpreted with the effect of change of the hydrogen bonding characteristics and the substitution pattern on structural variations of five membered rings from imidazolidinones 2 to pyrazoles 4 and pyrazolidinones 5, respectively. Therefore, it can be concluded that 4- phenyl-1-arylsulfonylimidazolidinone is a basic pharmacophore of imidazolidinones 2.
Subramanian, Santhosh,Sharma, Vinay K.,Yun, Jieun,Jung, Sang-Hun Korean Chemical Society 2014 Bulletin of the Korean Chemical Society Vol.35 No.10
To investigate the possible isosteric replacement of imidazolidinone moiety in 4-phenyl-1-arylsulfonylimidazolidinones (2) for broad and potent anti-cancer agents, a series of 5-phenyl-1H-pyrazol-3-yl 1-(acyl)indoline-5-sulfonates (4) and 1-(1-(acyl)indolin-5-ylsulfonyl)-5-phenylpyrazolidin-3-ones (5) were prepared and evaluated for their cytotoxicity against six human cancer cell lines. Although the pyrazoles 4 or pyrazolidinones 5 showed relatively good activity, still they showed lesser activity in comparison to imidazolidinones 2. These activity decreases could be interpreted with the effect of change of the hydrogen bonding characteristics and the substitution pattern on structural variations of five membered rings from imidazolidinones 2 to pyrazoles 4 and pyrazolidinones 5, respectively. Therefore, it can be concluded that 4-phenyl-1-arylsulfonylimidazolidinone is a basic pharmacophore of imidazolidinones 2.
M. Manhas,Vinay Kumar,Vivek K. Singh,J. Sharma,Ram Prakash,Vishal Sharma,A.K. Bedyal,H.C. Swart 한국물리학회 2017 Current Applied Physics Vol.17 No.11
The present paper reports on the structural and luminescent properties of un-doped and Sm3þ doped Ba2Ca(BO3)2 phosphors synthesized by the conventional solid state method. For structural characterizations, the X-ray diffraction, FTIR spectroscopy and Rietveld refinement method were used. The FTIR spectrum was composed of basic BO3 and BO4 structural units of borates. The Sm3þ doped phosphors under 402 nm (6H5/2/4L13/2) excitation, showed an orange red emission corresponding to the 601 nm (4G5/2 / 6H7/2) transition of the Sm3þ ion. An increase in the PL emission intensity was observed up to 2 mol % with the increase in Sm3þ ions concentration. The critical distance between the Sm3þ e Sm3þ ions were found to be 24.36 Å. Moreover, the phosphors decaytime and optical bandgap at different concentration of Sm3þ ion also have been discussed in details. All the results show that Ba2Ca(BO3)2:Sm3þ phosphor may be used with a near ultraviolet (n-UV) chip to fill the amber gap in light emitting diodes (LEDs).
Interleukin-5 저해 활성 chalcone 화합물의 유효 입체 구조
이기철,김민석,P. Thanigaimalai,Vinay K. Sharma,박경래,김영수,정상헌 충남대학교 약학대학 의약품개발연구소 2010 藥學論文集 Vol.25 No.-
Interleukin(IL)-5 appears to be one of the main proinflammatory mediators among the growing number of cytokines and chemokines that induce eosinophilic inflammation. Previously, our group synthesized a number of chalcone derivatives to determine their inhibitory activity against IL-5. However, the structure-activity relationship (SAR) of these chalcones was somewhat unclear, robably due to presence of three free rotatable bonds. To further, explore the SAR of these chalcones, we synthesized eight 2-(benzylidene)-2,3-dihydroinden-1-ones and 2- benzylidene)-3,4-dihydronaphthalen-1(2H)-ones 6 and evaluated for their inhibitory activity against IL-5. These rigidified chalcones 6 exhibited very weak inhibitory activity against IL-5 compared to chalcones 2. The structures of 6 closely resemble to the stretched conformations of chalcone 2, not effective conformation for the inhibition on IL-5 function.