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Acrosin structure-based design,synthesis and biological activities of 7-azaindol derivatives as new acrosin inhibitors

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Chinese Chemical Letters 2011年第3期22卷 272-275页

作者： Jun Hang Jiang Xue Fei Liu Can Hui Zhen You Jun Zhou Ju Zhu Jia Guo Lv chun quan sheng Department of Medicinal Chemistry School of Pharmacy Second Military Medical University Shanghai 200433 China

A series of 7-azaindol derivatives were designed based on the homologous 3D model of human *** compounds were synthesized and evaluated for their human acrosin inhibitory activities in *** 7a,7i,7j,7k and 7n showed highly inhibitory activity against human *** three-dimensional structure-activity relationship was investigated through a CoMFA model,which provided valuable information to further study of potential human acrosin inhibitors.

关键词： Rational design Azaindole Synthesis Acrosin CoMFA

Design, synthesis and molecular docking studies of novel triazole antifungal compounds

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Chinese Chemical Letters 2007年第6期18卷 663-666页

作者： Qiu Qin He Ke Li Yong Bing Cao Huan Wen Dong Li Hua Zhao Chao Mei Liu chun quan sheng School of Pharmacy Second Military Medical University Shanghai 200433 China

Based on the active site of Candida albicans lanosterol 14α-demethylase (CACYP51), novel triazole compounds structurally different from the current triazole drugs were designed and synthesized. In vitro antifungal activities showed that compounds 10, 11, 16 and 20 exhibited strong activities. In addition, compounds 10, 11 and 16 also displayed certain activities against fluconazole-resistant fungi.

关键词： Lanosterol 14α-demethylase Triazole tert-Butyl Antifungal activity Fluconazole-resistant

New triazole derivatives containing substituted 1,2,3-triazole side chains:Design,synthesis and antifungal activity

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Chinese Chemical Letters 2017年第4期28卷 913-918页

作者： Hai-Jiang Chen Yan-Juan Jiang Yong-Qiang Zhang Qi-Wei Jing Na Liu Yan Wang Wan-Nian Zhang chun-quan sheng School of Pharmacy Fujian University of Traditional Chinese Medicine School of Pharmacy Second Military Medical University School of Pharmacy East China University of Science and Technology

In order to discover new generation of triazole antifungal agents,a series of novel antifungal triazoles were designed and synthesized by structural simplification of our previously identified triazolepiperdine-heterocycle lead *** target compounds showed good antifungal activity with a broad *** particular,compound 71 was highly active against Candida albicans and Candida ***,compound 71 showed potent in vivo antifungal efficacy in the Caenorhabditis *** infection model.

关键词： Triazole derivatives Antifungal activities Click reaction Molecular docking CYP51

Synthesis and Antitumor Activity of 7-Substituted Derivatives of Homocamptothecin

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Chinese Chemical Letters 2006年第6期17卷 720-722页

作者： Zhen Yuan MIAO Wan Nian ZHANG Jian Zhong YAO chun quan sheng Yun Long SONG Hui XU Min ZHANG Jing ZHANG School of Pharmacy Second Military Medical University Shanghai 200433

Thirteen homocamptothecin derivatives were synthesized and in vitro antitumor activities were evaluated by the standard MTT method. The results showed that some of the homocamptothecin derivatives had higher antitumor... 详细信息

关键词： Antitumor activity homocamptothecin synthesis.

Total Synthesis of Phakellistatin 13 by Solution Method

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Chinese Chemical Letters 2006年第8期17卷 995-998页

作者： Qing Feng JIANG You Jun ZHOU Jian Zhong YAO Jia Guo LU Ju ZHU chun quan sheng Can Hui ZHENG Bing YAO Department of Medicinal Chemistry School of Pharmacy Second Military Medical University Shanghai 200433

Phakellistatin 13 is a good antitumor lead compound isolated from halobios. It was synthesized first time by solution method in combination of stepwise coupling and segment condensation. Final deprotection and cyclization were achieved according to our designed method, which was different from the reported process. The spectral data of synthetic product is consisted with literatureal data of natural product. Total synthesis of phakellistatin 13 is a significant achievement to further study of its derivatives and developing novel antitumor drugs.

关键词： Phakellistatin 13 solution-phase synthesis cyclopeptide.

Synthesis and antitumor activity of novel 10-amino acids ester homocamptothecin analogues

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Chinese Chemical Letters 2008年第7期19卷 811-813页

作者： Liang You Wan Nian Zhang Zhen Yuan Miao Wei Guo Xiao Ying Che Wen Ya Wang chun quan sheng Jiang Zhong Yao Ting Zhou School of Pharmacy Second Military Medical University Shanghai 200433 China

Nine racemic homocamptothecin derivatives were synthesized and in vitro antitumor activities were evaluated by standard MTT method. The results showed that some of the compound had higher antitumor activity than irite... 详细信息

关键词： Homocamptothecin Amino acids ester Antitumor activity Synthesis

Design,synthesis and antifungal activity of carbazole derivatives

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Chinese Chemical Letters 2014年第2期25卷 229-233页

作者： Shi-Ping Zhu Wen-Ya Wang Kun Fang Zheng-Gang Li Guo-Qiang Dong Zhen-Yuan Miao Jian-Zhong Yao Wan-Nian Zhang chun-quan sheng School of Pharmacy Second Military Medical University

The incidence of invasive fungal infections is increasing rapidly. Clinically available antifungal agents suffer from limited efficacy and severe resistance. There is an urgent need to discover antifungal lead compounds with novel chemical scaffold. On the basis of our previously identified tetrahydrocarbazole antifungal leads, the structure-activity relationship was further explored by modifying the scaffold and the side chains. Several targeted compounds showed potent activity against Candida species. Particularly, compound 13i showed better antifungal activity than the lead compound, which can be used as a good starting point for further optimization.

关键词： Carbazol Antifungal activity Structure-activity relationship

Amino acid derivatives of pyropheophorbide-a ethers as photosensitizer： Synthesis and photodynamic activity

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Chinese Chemical Letters 2016年第5期27卷 623-626页

作者： Zhi Meng Bin Shan Ling Zhang Gui-Yan Han Ming-Hui Liu Ning-Yang Jia Zhen-Yuan Miao Wan-Nian Zhang chun-quan sheng Jian-Zhong Yao Department of Medicinal Chemistry School of Pharmacy Second Military Medical University Shanghai 200433 China Department of Pharmacy Fujian University of Traditional Chinese Medicine Fuzhou 350122 China Department of Radiology Shanghai Eastern Hepatobiliary Surgery Hospital Second Military Medical University Shanghai 200438 China

Ten new water-soluble amino acid conjugates of pyropheophorbide-a ethers 4a-4J were synthesized and investigated for their in vitro photodynamic antitumor activity. The results showed that all compounds exhibited higher phototoxicity and lower dark toxicity against three kinds of tumor cell lines than BPD-MA. In particular, the most phototoxic compound 4d and 4j individually showed ICso values of 41 nmol/L and 33 nmol/L against HCT116 cell, which represented 7.8- and 9.7-fold increase of antitumor potency compared to BPD-MA, respectively, suggesting that they were promising photosensitizers for PDT applications because of their strong absorption at long wavelength （λmax 〉 650 nm）, high phototoxicitv, low dark cvtotoxicitv and ~ood water-solubility.

关键词： Photodynamic therapy (PDT) Photosensitiser Pyropheophorbide-α Chlorin Antitumor

Design, synthesis and biological evaluation of E-ring modified evodiamine derivatives as novel antitumor agents

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Chinese Chemical Letters 2014年第7期25卷 978-982页

作者： Kun Fang Guo-Qiang Dong Hai Gong Na Liu Zhen-Gang Li Shi-Ping Zhu Zhen-Yuan Miao Jian-Zhong Yao Wan-Nian Zhang chun-quan sheng School of Pharmacy Second Military Medical University Department of Radiation Oncology Ji’nan Military General Hospital

A series of novel E-ring modified evodiamine derivatives were designed and synthesized as antitumor agents. Their capacity to interfere with the catalytic activity of topoisomerase Ⅰ and Ⅱ was evaluated by the relaxation assay. In vitro antitumor activity results revealed that compound 12 showed good antitumor activity with a broad spectrum. Its binding modes with topoisomerase Ⅰ and Ⅱ were clarified by molecular docking.

关键词： Evodiamine derivatives Topoisomerase Ⅰ Topoisomerase Ⅱ Antitumor activity