نتایج جستجو برای: inhibitory concentration 50

تعداد نتایج: 882418  

2011
Chad Brown Tammy M. Havener Lorraine Everitt Howard McLeod Alison A. Motsinger-Reif

Cytotoxicity assays of immortalized lymphoblastoid cell lines (LCLs) represent a promising new in vitro approach in pharmacogenomics research. However, previous studies employing LCLs in gene mapping have used simple association methods, which may not adequately capture the true differences in non-linear response profiles between genotypes. Two common approaches summarize each dose-response cur...

Journal: :The Journal of antibiotics 1998
M Speitling P Nattewan K Yazawa Y Mikami I Grün-Wollny M Ritzau H Laatsch U Gräfe

New anthracycline antibiotics 3'-O-demethyl mutactimycin (3) and 4-O,3'-O-didemethyl mutactimycin (4) were isolated from two actinomycetes strains, Nocardia transvalensis and Streptomyces sp. GW 60/1571. The chemical structures were elucidated by mass spectrometry and NMR spectroscopy. Antibiotic 3 displayed moderate antimicrobial activity against Gram-positive bacteria and cytotoxicity against...

Journal: :Dalton transactions 2014
Benjamin J Pages Feng Li Paul Wormell Dale L Ang Jack K Clegg Cameron J Kepert Lawson K Spare Supawich Danchaiwijit Janice R Aldrich-Wright

Eight platinum(II) complexes with anticancer potential have been synthesised and characterised. These complexes are of the type [Pt(I(L))(A(L))](2+), where I(L) is either dipyrido[3,2-f:2',3'-h]quinoxaline (dpq) or 2,3-dimethyl-dpq (23Me2dpq) and A(L) is one of the R,R or S,S isomers of either 1,2-diaminocyclohexane (SS-dach or RR-dach) or 1,2-diaminocyclopentane (SS-dacp or RR-dacp). The CT-DN...

Journal: :Journal of natural products 2015
Chung Sub Kim Lalita Subedi Sun Yeou Kim Sang Un Choi Ki Hyun Kim Kang Ro Lee

Phytochemical investigation of the twigs of Chaenomeles sinensis led to the isolation and identification of six new lignan glycosides, chaenomiside A-F (1-6), along with five known ones (7-11). Their chemical structures were determined by spectroscopic methods, including NMR, MS, ECD, and GC/MS analyses. All the isolated compounds (1-11) were tested for their inhibitory effects on nitric oxide ...

2006
Yutaka Koguchi Jun Kohno Maki Nishio Kohei Takahashi Toru Okuda Tetsuo Ohnuki Saburo Komatsubara

In our course of screening for novel proteasome inhibitors, TMC-95A and its diastereomers, TMC-95Bto D, were isolated from the fermentation broth of Apiospora montagnei Sacc. TC 1093. TMC-95Ainhibited the chymotrypsin-like (ChT-L), trypsin-like (TL), and peptidylglutamyl-peptide hydrolyzing (PGPH) activities of 20S proteasome with IC50 values of 5.4nM, 200nM, and 60nM, respectively. TMC-95Binhi...

Journal: :Molecules 2018
Tianxiao Wu Yu Pang Jing Guo Wenbo Yin Mingyue Zhu Chenzhou Hao Kai Wang Jian Wang Dongmei Zhao Maosheng Cheng

A series of novel 2,4-diaminoquinazoline derivatives were designed, synthesized, and evaluated as p21-activated kinase 4 (PAK4) inhibitors. All compounds showed significant inhibitory activity against PAK4 (half-maximal inhibitory concentration IC50 < 1 μM). Among them, compounds 8d and 9c demonstrated the most potent inhibitory activity against PAK4 (IC50 = 0.060 μM and 0.068 μM, respectively)...

2015
Ting-Hsi Hsiao Chun-Sung Sung Yu-Hsuan Lan Yi-Chen Wang Mei-Chin Lu Zhi-Hong Wen Yang-Chang Wu Ping-Jyun Sung Anake Kijjoa

Two new cembranes, columnariols A (1) and B (2), were isolated from the cultured soft coral Nephthea columnaris. The structures of cembranes 1 and 2 were elucidated by spectroscopic methods. In the anti-inflammatory effects test, cembranes 1 and 2 were found to significantly inhibit the accumulation of the pro-inflammatory iNOS and COX-2 protein of the lipopolysaccharide (LPS)-stimulated RAW264...

2013
Uli Kazmaier Angelika Ullrich Judith Hoffmann

Tubulysins, linear tetrapeptides produced by several strains of myxobacteria, show an extremely high toxicity towards a wide range of cancer cell lines, with IC50 values in the nano or even picomolar range. Therefore, tubulysins and their derivatives might be suitable candidates for the development of antitumor drugs. Several synthetic approaches for tubulysins and derivates have been developed...

Journal: :The Journal of antibiotics 1998
N Morisaki Y Mitsui Y Yamashita Y Koiso R Shirai Y Hashimoto S Iwasaki

Ustiloxin D, produced by the rice plant pathogen Ustilaginoidea virens, exhibits potent anti-tubulin activity. In order to elucidate the effects of functional groups in ustiloxin D on its activity, several derivatives were synthesized and their anti-tubulin activities were estimated. The N,N-dimethylamino derivative and the 14-O-methyl derivative were inactive (IC50 > 50 microM). 20-Hydroxymeth...

Journal: :Molecules 2017
Huai Xiao Tian-Peng Yin Jian-Wei Dong Xiu-Mei Wu Qing Luo Jian-Rong Luo Le Cai Zhong-Tao Ding

Five new phenolic compounds rynchopeterines A-E (1-5), in addition to thirteen known phenolics, were isolated from Blaps rynchopetera Fairmaire, a kind of medicinal insect utilized by the Yi Nationality in Yunnan Province of China. Their structures were established on the basis of extensive spectroscopic analyses (1D and 2D NMR, HR-MS, IR) along with calculated electronic circular dichroism met...

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