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1. Synthesis and Biological Evaluation of Novel β-Carboline Derivatives as Antiproliferative Agents | |||
Jing Chen,Wenting Du,Xuefen Tao,Jiawei Huang,Yuliang Song | |||
Pharmacy 07 July 2013 | |||
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Abstract:A series of novel β-carboline derivatives were synthesized and evaluated for their cytotoxic activities in vitro against two human tumor cell lines. Many of the compounds showed moderate to potent cytotoxic activities against the tested cell lines, in which compound 12l exhibited the most potent antiproliferative activities against KB cell line (IC50 = 4.58 μM). Preliminary mechanism research on compound 12l indicated it could inhibit DNA intercalation and tubulin polymerization. | |||
TO cite this article:Jing Chen,Wenting Du,Xuefen Tao, et al. Synthesis and Biological Evaluation of Novel β-Carboline Derivatives as Antiproliferative Agents[OL].[ 7 July 2013] http://en.paper.edu.cn/en_releasepaper/content/4545993 |
2. Synthesis and Cytotoxicity of Novel 20-O-linked (±)-Homocamptothecin Ester Derivatives | |||
LI Dizao,Pan Xiandao | |||
Pharmacy 05 June 2013 | |||
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Abstract:(±)-Homocamptothecin (hCPT) is a semisynthetic analogue of camptothecin (CPT) with a seven-membered β-hydroxylactone resulting from the insertion of a methylene (-CH2-) spacer between the alcohol moiety and the carboxyl group of the classical six-membered α-hydroxylactone ring of CPT. This E-ring modification provides a less reactive lactone with enhanced stability and decreased protein binding in human plasma and rather appears to improve instead of impairing its activity against topoisomerase I (Topo I) compared to CPT. In an attempt to improve the antitumor activity of homocamptothecins, a series of novel 20-O-linked hCPT ester derivatives were first designed and synthesized based on a synthetic route which acylates semi-synthesized (±)-homocamptothecin with different substituted phenoxyacetic acid ester derivatives. Most of the synthesized hCPT ester derivatives were assayed for in vitro cytotoxicity against six human cancer cell lines KB, KB/VCR, A549, HCT-8, Bel7402 and A2780 and most of the assayed compounds exhibited good antiproliferative activity on these tumor cell lines especially on KB. Here the synthesis and the in vitro antitumor evaluation of 20-O-linked substituted phenoxyacetic acid ester derivatives of (±)-hCPTs are reported. | |||
TO cite this article:LI Dizao,Pan Xiandao. Synthesis and Cytotoxicity of Novel 20-O-linked (±)-Homocamptothecin Ester Derivatives[OL].[ 5 June 2013] http://en.paper.edu.cn/en_releasepaper/content/4545343 |
3. Comparative studies of paeoniflorin and albiflorin from Chinese Paeony on Anti-inflammatory activities | |||
GAO Teng,WANG Qiangsong,CUI Yuanlu | |||
Pharmacy 20 May 2013 | |||
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Abstract:Purpose: Chinese Paeony has been used for more than 1000 years in traditional Chinese medicine for the treatment of gynecological problems, cramp, pain, giddiness, and congestion. Paeoniflorin and albiflorin, monoterpene glycosides isolated from Chinese Paeony, possess a variety of pharmacological activities. The present study was investigated the anti-inflammatory activities of paeoniflorin and albiflorin using models of Lipopolysaccharides (LPS) induced RAW 264.7 cells. Methods: Production of nitric oxide (NO) was measured by the Griess colorimetric method and (ELISA). In addition, interleukin 6 (IL-6) and tumor necrosis factor alpha (TNF-α) synthesis were analyzed using enzyme-linked immunosorbent assay (ELISA). The protein expression of cyclooxygenase-2 (COX-2) was detected by cell-based ELISA. The gene expression levels of inducible nitric oxide synthase (iNOS), COX-2, TNF-α, IL-6 were detected by quantitative real-time reverse-transcription polymerase chain reaction (real-time RT-PCR). Results: The results showed that paeoniflorin and albiflorin could inhibit LPS-induced NO, TNF-α, IL-6 production and protein expression of COX-2. Furthermore, they could inhibit the mRNA expression of inducible nitric oxide synthase (iNOS), cyclooxygenase-2 (COX-2), TNF-α, IL-6. Conclusion: These results show that albiflorin has the similar pharmacological effects to paeoniflorin on anti-inflammatory activities, which will provide a new evidence to pay albiflorin more attention to main quality control indicators of Paeoniae Radix and edit the new Chinese Pharmacopoeia. | |||
TO cite this article:GAO Teng,WANG Qiangsong,CUI Yuanlu. Comparative studies of paeoniflorin and albiflorin from Chinese Paeony on Anti-inflammatory activities[OL].[20 May 2013] http://en.paper.edu.cn/en_releasepaper/content/4544036 |
4. CYP3A4 and CYP3A5 Polymorphism Effects on Tacrolimus Pharmacokinetics in Chinese Adult Renal Transplant Recipients: A Population Pharmacokinetic Analysis | |||
ZUO Xiaocong,Chee M. Ng,Jeffrey S.Barrett,LUO Aijing,ZHANG Bikui,DENG Chenhui,XI Lanyan,CHENG Ke,MING Yingzi,YANG Guoping,PEI Qi,ZHU Lijun,YUAN Hong,LIAO Haiqiang,DING Junjie,WU Di,ZHOU Yanan,JING Ningning,HUANG Zhijun | |||
Pharmacy 25 April 2013 | |||
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Abstract:Objective Tacrolimus is used clinically for long-term treatment of antirej |