Chinese︱Feedback︱Save this page

Login︱Register

• Elaborating Academic Views 　　　　 • Exchanging Innovative Ideas
• Protecting Intellectual Properties 　　• Fast Sharing Science Papers

Sponsored by the Center for Science and Technology Development of the Ministry of Education
Supervised by Ministry of Education of the People's Republic of China

Home > Papers > Medicinal-Chemistry

There are 45 papers published in subject: > since this site started.

Results per page:

45 Total, 5 Pages | << First < Previous 1 2 3 4 5 Next > Last >>

Select Subject

All (8828)

Agronomy (158)

Animal Husbandry,... (64)

Aquatic Science (16)

Astronomy (36)

Aviation (22)

Basic Medicine (184)

Biology (504)

Chemical Engineering (103)

Chemistry (635)

Civil and Archite... (105)

Clinical Medicine (236)

Computer Science ... (924)

Dynamic and Elect... (121)

Earth Science (119)

Economics (67)

Education (31)

Electrics, Commun... (927)

Energy Science an... (67)

Engineering and T... (15)

Environmental Sci... (140)

Food Science and ... (63)

Forestry (36)

Hydraulic Enginee... (40)

Mechanics (240)

Metallurgical Eng... (32)

Mine Engineering ... (38)

Nuclear Science a... (21)

Pharmacy (98)

Physics (920)

Preventive Medici... (37)

Psychology (20)

Security Science ... (17)

Sports Science (6)

Surveying and Map... (15)

Textile Science a... (16)

Traditional Chine... (56)

Transportation En... (57)

Third-level Subject

Rank

Results per page:

45 Total, 5 Pages | << First < Previous 1 2 3 4 5 Next > Last >>

Alert Name:
Alerting to:
Authentication email will be sent to your email address in 24 hours
Frequency:
Email Message Format:	Plain text Graphical(HTML)

Complete the form below and we will recommend the selected titles to your friends on your behalf. * Indicates a required field.
Your name*:
Your email address*:
Recipient's name*:
Recipient's email address*:
(multiple recipient's names and email addresses should be separated with semicolons)
Your comments:	I thought you would find the page(s) useful.

Your name:
Your email address:
Recipient's name:
Recipient's email address:
(multiple recipient's names and email addresses should be separated with semicolons)
Your comments:	I thought you would find this page useful.

Disclaimer: This message was sent to your friend using the "Send it to a friend" facility on the Sciencepaper Online’ WWW site, http://www.paper.edu.cn/en. The Sciencepaper Online is not responsible for the content of this email, and anything said in this email does not necessarily reflect the Sciencepaper Online's views.


	1. Synthesis, Crystal Structure and Theoretical Study of Novel Bromoquinoline
	REN Yu,CUI Sheng-Feng,GENG Rong-Xia,ZHOU Cheng-He
	Pharmacy 26 February 2014
	Show/Hide Abstract \| Cite this paper︱Full-text: PDF (0 B)

	Abstract:A new 4-bromo-6,8-difluoro substituted quinoline derivative 3 was synthesized and characterized by IR, 1H NMR, MS and X-ray single-crystal diffraction. The target compound crystallized in a orthorhombic system, space group Pbca with a = 13.6139(3), b = 13.6440(3), c = 17.4199(4) ?, α = 90.000(2), β = 90.000(2), γ = 90.000(2) , V = 3235.71(13) ?3, Z = 8, C14H11N2OF2Br3, Mr = 500.96, F(000) = 1920, Dc = 2.057 g/cm3, μ = 9.47 mm?1, R = 0.040 and wR = 0.103 for 2888 independent (Rint = 0.026) and 2463 observed (I > 2σ(I)) reflections. In this crystal, one of the Br atoms on the alkyl chain was disordered over two positions with refined occupancies of 0.8698(1) and 0.1301(9). The calculated geometrical parameters of this compound were consistent with the experimental values. This compound possessed moderate antimicrobial activity.
	TO cite this article:REN Yu,CUI Sheng-Feng,GENG Rong-Xia, et al. Synthesis, Crystal Structure and Theoretical Study of Novel Bromoquinoline[OL].[26 February 2014] http://en.paper.edu.cn/en_releasepaper/content/4587493


	2. Synthesis, Characterization, and Crystal Structures of Propargyl Naphthalimides
	PENG Li-Ping,LV Jing-Song,ZHOU Cheng-He
	Pharmacy 26 February 2014
	Show/Hide Abstract \| Cite this paper︱Full-text: PDF (0 B)

	Abstract:Two title molecules, 6-bromo-2-(prop-2-ynylamino)-1H-benzo[de]isoquinoline -1,3(2H)-dione (4) and 6-bromo-2-(diprop-2-ynylamino)-1H-benzo[de]isoquinoline-1,3(2H)-dione (5), were synthesized and characterized by single-crystal X-ray diffraction, IR, 1H NMR, MS, fluorescence spectra, and powder X-ray diffraction (PXRD). The structure of crystal 4 (CCDC 981232) belongs to the triclinic system, space group P-1 with a = 7.5827(5), b = 7.8886(6), c = 10.5217(7) ?, α = 96.368(6), β = 90.223(5), γ = 92.353(6)o, V = 624.95(7) ?3, Dc = 1.749 g/cm3, μ = 4.52 mm-1, F(000) = 328, Rint = 0.0260, R (I > 2σ(I)) = 0.0622, wR (I > 2σ(I)) = 0.1454, R (all data) = 0.0683 and wR (all data) = 0.1484. In this crystal, a 2D layer supramolecular network structure was formed through hydrogen bonds of N(2)?H(2)oooO(1) and C(15)?H(15)oooO(1), and the Br atom was disordered over two positions with refined occupancies of 0.8589(3) and 0.1410(7). The calculated bond lengths and bond angles of compound 4 were consistent with the result of crystallography. Fluorescence properties of compounds 4 and 5 in different solvents were also studied. Moreover, the two synthesized compounds 4 and 5 were screened for their antimicrobial activities against seven bacteria and four fungi. Bioactive assay manifested that the two compounds exhibited moderate antibacterial and antifungal activities against the tested strains in comparison with the reference drugs norfloxacin, chloromycin and fluconazole.
	TO cite this article:PENG Li-Ping,LV Jing-Song,ZHOU Cheng-He. Synthesis, Characterization, and Crystal Structures of Propargyl Naphthalimides[OL].[26 February 2014] http://en.paper.edu.cn/en_releasepaper/content/4587490

Saved Papers

Saved Papers


	3. Synthesis and biological evaluation of cytotoxic activity of 14-(β-D-2-deoxy-ribopyranosyl)-naphtho [2,1-a]pyrrolo[3,4-c]carbazole-5,7(6H,12H)-dione
	DING Ning
	Pharmacy 20 January 2014
	Show/Hide Abstract \| Cite this paper︱Full-text: PDF (0 B)

	Abstract:Naphtho[2,1-a]pyrrolo[3,4-c]carbazole-5,7(6H,12H)-dione (NPCD) is known to be a very potent and selective cyclin D1-CDK4 inhibitors and could induce strong G1 phase arrest in breast tumor cell lines. In this work, the synthesis and biological evaluation of cytotoxic activity of a novel NPCD glycoside, 14-(α-L-rhamnopyranosyl)-naphtho[2,1-a]pyrrolo[3,4-c] carbazole-5,7 (6H,12H)- dione (1) were reported. The results showed the NPCD glycoside 1 displayed strong tumor cell growth inhibitory activities in the range of micromolar IC50 towards a broad spectrum of tumor cell lines. Analysis of cell cycle profiles revealed that NPCD glycoside 1 arrested the cells at different phases depending on the cell lines.)
	TO cite this article:DING Ning. Synthesis and biological evaluation of cytotoxic activity of 14-(β-D-2-deoxy-ribopyranosyl)-naphtho [2,1-a]pyrrolo[3,4-c]carbazole-5,7(6H,12H)-dione[OL].[20 January 2014] http://en.paper.edu.cn/en_releasepaper/content/4583216


	4. Selective bromination of toluidines and cresols with N-bromosuccinimide
	Fang Xubin,Fang Lei
	Pharmacy 19 December 2013
	Show/Hide Abstract \| Cite this paper︱Full-text: PDF (0 B)

	Abstract:Using N-bromosuccinimide (NBS) as a convenientbromine source, bromination of toluidine and cresols was studied systematically to clarify the underlying mechanism and the orientation effect. Based on this methodology, several potential AChE inhibtors i.e. 3-bromo-2-methoxy-5-methyl-9H-carbazole, 3,6-dibromo-2-meth-oxy-5- methyl- 9H-carbazole, and 5-(bromomethyl)- 2-methoxy-9-(phenylsulfonyl)carbazole were synthesized.
	TO cite this article:Fang Xubin,Fang Lei. Selective bromination of toluidines and cresols with N-bromosuccinimide[OL].[19 December 2013] http://en.paper.edu.cn/en_releasepaper/content/4576050


	5. 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
	Show/Hide Abstract \| Cite this paper︱Full-text: PDF (0 B)

	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


	6. Synthesis and Cytotoxicity of Novel 20-O-linked (±)-Homocamptothecin Ester Derivatives
	LI Dizao,Pan Xiandao
	Pharmacy 05 June 2013
	Show/Hide Abstract \| Cite this paper︱Full-text: PDF (0 B)

	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


	7. Scaffold Evaluation of Liguzinediol Analogs as Novel Cardiotonic Agents
	LIU Zheng,LI Wei,QIN Kai,WEN Kan,ZHU Chenjian,LI Nianguang,BIAN Huimin,WEN Hongmei,CHEN Long
	Pharmacy 18 April 2013
	Show/Hide Abstract \| Cite this paper︱Full-text: PDF (0 B)

	Abstract:Liguzinediol (LZDO) could mediate the positive inotropic effects through sarcoplasmic reticulum Ca2+ ATPase-dependent mechanism without the risk of arrhythmia. However, the pharmacophore of LZDO contributed to the activities was not clear. The aim of this work is to explore the relationship between positive inotropic effect and scaffold of LZDO as well as to check whether the pharmacophore of LZDO on anti-heart failure activity was located at the pyrazine ring. A series of LZDO analogs (3a-b, 4a-b, 9-19) were designed and synthesised, and their activities were evaluated on isolated heart contractility by Langendorff perfusion. The results showed that the efficacy of LZDO was reduced when the hydroxyl, carboxyl or ester moieties at the side chain position of LZDO were induced, and the para-dihydroxy in LZDO was necessary for its activity. Thus, the pharmacophore of positive inotropic effect might be located at the whole scaffold of LZDO, but not at the pyrazine ring. The finding may provide important clue of pharmacophore for the development of novel cardiotonic agents.
	TO cite this article:LIU Zheng,LI Wei,QIN Kai, et al. Scaffold Evaluation of Liguzinediol Analogs as Novel Cardiotonic Agents[OL].[18 April 2013] http://en.paper.edu.cn/en_releasepaper/content/4538513


	8. Synthesis,Biological Evaluation,and Pharmacokinetic Study of Novel Liguzinediol Prodrugs
	LIU Zheng,LI Wei,WEN Hongmei,BIAN Huimin,CHEN Long,ZHANG Jing,CHEN Lei,YANG Kundi,FANG Qiuyue,CHEN Jing,FEI Yao
	Pharmacy 18 April 2013
	Show/Hide Abstract \| Cite this paper︱Full-text: PDF (0 B)

	Abstract: Liguzinediol (LZDO) ester prodrugs (3, 4, 5) were synthesized and evaluated in vitro and in vivo for its potential use, with the aim of prolonging the half-life of the parent drug LZDO (1a) in vivo. Prodrug 3, 4, 5 were found to be a potent positive inotropic effect on the myocardium without the risk of arrhythmia. Prodrug 3, 4, 5 rapidly underwent enzymatic hydrolysis to release the parent compound LZDO in 1-3 h in rat liver microsomes and rat plasma. The half-life of the parent compound was prolonged after intragastric administering prodrug 3. Prodrug 3 was found to be a superior prodrug candidate for increasing myocardial contractility.
	TO cite this article:LIU Zheng,LI Wei,WEN Hongmei, et al. Synthesis,Biological Evaluation,and Pharmacokinetic Study of Novel Liguzinediol Prodrugs[J].


	9. Design,synthesis and biological evaluation of novel asymmetric monocarbonyl analogues of curcumin (MACs ) as anti-inflammatory agents
	ZHANG Yali,ZOU Peng,ZHAO Chengguang,LIANG Guang,YANG Shulin
	Pharmacy 09 March 2013
	Show/Hide Abstract \| Cite this paper︱Full-text: PDF (0 B)

	Abstract:In the past several years, a lot of symmetric mono-carbonyl analogues of curcumin (MACs) have been designed and synthesized in our laboratory. In the recent study, Eleven asymmetric MACs were designed and synthesized. Their bioactivities were evaluated by inhibit LPS-stimulated macrophages release proinflammation cytokines TNF-α and IL-6. The compound 1d exhibit the most inhibit activity among the test compounds. These data show that asymmetric MACs might serve as potential agents for the treatment of inflammatory diseases.
	TO cite this article:ZHANG Yali,ZOU Peng,ZHAO Chengguang, et al. Design,synthesis and biological evaluation of novel asymmetric monocarbonyl analogues of curcumin (MACs ) as anti-inflammatory agents[OL].[ 9 March 2013] http://en.paper.edu.cn/en_releasepaper/content/4528456


	10. Synthesis and cytotoxicity of 3-arylacrylic ester derivatives of the simplified saframycin-ecteinascidin skeleton prepared from L-dopa
	DONG Wenfang,GUO Ju,LIU Wei,YAN Zheng,WANG Nan,LIU Zhanzhu
	Pharmacy 08 March 2013
	Show/Hide Abstract \| Cite this paper︱Full-text: PDF (0 B)

	Abstract:Fifteen simplified tetrahydroisoquinoline analogues were prepared from L-dopa. The in vitro antitumor activities of these analogues were evaluated against HCT-8, BEL-7402, BGC-823, A549, A2780, MCF-7 and MX-1 cell lines. The IC50 values of the cytotoxicity of most analogues were at the level of 10-7M or 10-8M. Compound 17 with 2,3,4-trimethoxycinnamate side chain at C-22 showed the most potent antitumor activity.
	TO cite this article:DONG Wenfang,GUO Ju,LIU Wei, et al. Synthesis and cytotoxicity of 3-arylacrylic ester derivatives of the simplified saframycin-ecteinascidin skeleton prepared from L-dopa[OL].[ 8 March 2013] http://en.paper.edu.cn/en_releasepaper/content/4527983

	Check out RSS, or use RSS reader to subscribe this item