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Synthesis and Antitumor Activity of New Anthracycline Analogues
김완중,유동진,강현수,장순량,Kim, Wan Jung,Yu, Dong Jin,Gang, Hyeon Su,Jang, Sun Ryang 대한화학회 2001 Bulletin of the Korean Chemical Society Vol.22 No.9
New anthracycline analogues 2-9 as potential anticancer agents have been synthesized from daunomycin (1a) and doxorubicin (1b). Compounds 2 and 6 were prepared by the nucleophilic displacement type esterification of 14-bromodaunomycin (1c) with N-benzoyl-(2R,3S)-phenylisoserine and L-pyroglutamic acid in triethyl-amine, respectively. Compounds 3, 7 and 4, 8 were prepared by the reaction of either daunomycin (1a) or doxorubicin (1b) with one equivalent of the corresponding acids in the presence of EDCI/PP. Compounds 5, 9 were obtained from 1b by reaction with 2.2 equivalents of the corresponding acids in the same manner. The cytotoxic activities of the analogues in comparison with adrimycin on cultured SNU-16 and MCF7 cell were described.
Synthesis of New Anthracycline Derivatives Including Butyric or Retinoic Acid Moiety.
김완중,박시호,유동진,강흔수,정순량,Kim, Wan Jung,Park, Si Ho,Yu, Dong Jin,Gang, Heun Su,Jeong, Sun Ryang 대한화학회 2001 Bulletin of the Korean Chemical Society Vol.22 No.6
The potential anticancer agents, new anthracycline analogues (2-9) have been synthesized from the glycosides daunomycin (1a) and doxorubicin (1b). Compounds 2 and 6 were prepared by nucleophilic displacement esterification of a 14-bromodauomycin(1c) with sodium or potassium salts of butyric and all trans retinoic acid, respectively. Compounds 3 and 7 were obtained from daunomycin (1a) by direct amidation with a butyric and all trans retinoic acid in the presence of EDCI and PP, respectively. Compounds 4 and 8 were obtained from doxorubicin (1b) by reaction with the corresponding acids in the same manner. Compounds 5 and 9 were prepared from doxorubicin (1b) by acylation with two equivalents of the corresponding acids under the same reaction conditions.
Synthesis of New Anthracyline Derivatives Containg Acetylsalicyclic or Palmitic Acid Moiety.
김완중,박시호,유동진,강흔수,정순량,Kim, Wan Jung,Park, Si Ho,Yu, Dong Jin,Gang, Heun Su,Jeong, Sun Ryang 대한화학회 2001 Bulletin of the Korean Chemical Society Vol.22 No.6
The potential anticancer agents new anthracycline derivatives (2~9) have been synthesized from daunomycin (1a) and doxorubicin (1b) ad starting materials. Compounds 2 and 6 were prepared by the nucleophilic displacement type esterification of a 14-bromodaunomycin (1c) with a acetylsalicylic and palmitic acid in triethylamine, respectively. Compound 3 and 7 were obtained from daunomycin (1a) by direct amidation with the corresponding acids in the presence of EDCI and PP as esterification regents. Whereas 4 and 8 were prepared by reaction of doxorubicin (1b) with one equivalent of acetylsalicylic and palmitic acid using DCC/DMAP, respectively, 5 and 9 were obtained from 1b by acylation with two equivalents of the corresponding acids using EDCI/PP reagents.
김완중(Wan Jung Kim),김중남(Jung Nam Kim),김호중(Ho Jung Kim),문철웅(Chul Oong Moon),이승일(Soung Il Lee),장경식(Kyoung Sig Chang),홍순표(Soon Pyo Hong) 대한내과학회 1990 대한내과학회지 Vol.39 No.4
N/A Heart rate variability is a noninvasive index of the neural, especially parasympathetic, activity of the heart. Autonomic neuropathy is frequently observed in diabetic patients, and a 5-year survival rate of this kind of patient is low. To evaluate autonomic neuropathy in diabetic patients, 35 diabetic patients (proliferative retinopathy: 14, neurogenic bladder:8, postural hypotenion:6) measured for RR intervals and Valsalva ratios compared with 77 persons of the normal control group. RR variations (standard deviation: SD, coefficient of variation: CV, max-min, max/min) during deep respiration and Valsalva ratios (Vmax-Vmin, Vmax/Vmin) during Valsalva maneuver were significantly lower in the diabetic patients than in the normal control group (p<0.001, respectively). RR variations and Valsalva ratios decreased progressively with an increase of age in the control group and in diabetic patients (p<0.001, respectively). RR variations and Valsalva ratios were significantly lower in the diabetic patients with retinopathy, neurogenic bladder, and postural hypotension compared to diabetic patients without such conditions (P value <0.01, <0.05, <0.05, respectively). It is concluded that diabetic autonomic neuropathy can be indicated by the measurement of RR variations and Valsalva ratios.
김완중(Wan-Jung Kim),최창호(Chang-Ho Choi),현동석(Dong-Seok Hyun) 전력전자학회 1998 전력전자학술대회 논문집 Vol.- No.-
Under high power IGBTs switching, a large overvoltage is induced across the IGBT module due to the stray inductance in the circuit. This paper proposes a new gate drive circuit for high power IGBTs which can actively suppress the overvoltage across the driven IGBT at turn-off while preserving the most simple and reliable power circuit. The turn-off driving scheme has adaptive feature to the amplitude of collector current, so that the overvoltage can be limited much effectively at the fault collector current. Experimental results under various normal and fault conditions prove the effectiveness of the proposed.<br/> <br/>
대장암에서 종양억제 유전자와 p53의 상위조절인자로서의 hSRBC 연구
김완중 ( Wan Jung Kim ),김효종 ( Hyo Jong Kim ),지성길 ( Sung Gil Chi ),김진오 ( Jin Oh Kim ),조주영 ( Joo Young Cho ),심찬섭 ( Chan Sup Shim ) 대한장연구학회 2007 Intestinal Research Vol.5 No.2
Background/Aims: hSRBC [human Serum deprivation response (sdr)-Related gene product that Binds to c-kinase] was identified using PKCδ or BRCA1 as a probe and located at 11p15.5-p15.4 region. Expression of hSRBC protein was also decreased in a number of breast, lung, and ovarian cancer cell lines, suggesting that hSRBC might be a putative tumor suppressor gene. Methods: The expression status of hSRBC was analyzed in 50 primary colon tumors and their adjacent 50 normal tissues, and 20 colon cancer cell lines. Transcript and protein expression of hSRBC was studied by quantitative RT-PCR and Western blot, respectively. siRNA-mediated knockdown of hSRBC expression was utilized to investigate its association with p53. Results: The mRNA expression of hSRBC was decreased in 60% (12/20) of colon cancer cell lines and 44% (22/50) of patient``s colon cancer tissues. Expression of hSRBC mRNA was significantly decreased in tumors compared to non-cancerous cells, while genomic level of hSRBC was not decreased in tumors. hSRBC expression was increased by 5-aza-2’-deoxycytidine treatment and hypermethylation of CpG sites was strongly associated with decreased expression. Ectopic transfection of hSRBC suppressed RKO cell count and hSRBC knockdown by siRNA augmented HCT116 cell numbers. Flow cytometry showed G1 arrest and apoptosis of colon cancer cells by restoration of hSRBC expression in RKO cells. Both basal and etoposide-mediated p53 expression was decreased when hSRBC expression was knockdowned with siRNA. Conclusions: hSRBC expression is frequently decreased by promoter CpG site hypermethylation. hSRBC down-regulates p53 expression in G1 phase and might be a novel upstream regulator of p53. (Intest Res 2007;5:131-143)