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进行了动物体内抗肿瘤活性研究的多为天然药物,但其来源有限;虽然用于抗肿瘤研究的合成化合物种类较多,但对于其在动物体内抗肿瘤研究又相对偏少,所以,合成化合物抗肿瘤体内研究已经成为研究热点之一。本文对合成化合物抗肿瘤作用机制、体内肿瘤模型建立方法和体内抑瘤实验研究等方面的研究进展进行了评述,并通过大量实验数据对合成化合物毒性评价方法、抑瘤基本观察指标测定、氧化损伤相关酶活力的测定方法、组织病理学评价方法等体内抑瘤实验的评价标准和方法进行了详细总结,提出了合成化合物在体内动物抗肿瘤实验研究方法中亟待解决的问题,为新型抗肿瘤合成化合物体内药学活性研究提供有益的参考。 相似文献
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Our research improves the structure diversity of naphthalimide antitumor agents and distinct variances of antitumor targets and mechanism of action. 相似文献
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Development of drug delivery systems for cancer therapy is a crucial issue. Previously, some peptides were designed as tumor homing cell-penetrating peptides with antitumor activities. In this study, dual function dendrimers with tumor targeting activities and antitumor effects were designed using the tumor targeting CPP44 peptide for acute myelogenous leukemia (AML) and the antitumor p16INK4a peptide. Two types of peptide–dendrimer conjugates were synthesized. One was a CPP44-linked p16INK4a peptide-conjugated dendrimer (tandem linked dendrimer) and the other was a dendrimer conjugated with separate CPP44 and p16INK4a peptides (parallel linked dendrimer). In addition, a peptide cathepsin B substrate was linked to the antitumor p16INK4a peptide to release it from the carriers. These peptide–dendrimer conjugates produced more effective antitumor effects than a CPP44-linked p16INK4a peptide. The parallel linked dendrimer showed less association with AML cells than the tandem linked dendrimer, but had greater antitumor effects. This suggested that both cellular uptake and antitumor peptide cleavage affected the antitumor activities of dual functional peptide-conjugated dendrimers. 相似文献
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This study researches the synthesis of Arginine-Glycine-Asparti (RGD) peptide modification of copolymer: poly (lactic acid-co-L-lysine) (PLA-PLL-RGD) and the preparation of mitoxantrone (DHAQ)-loaded PLA-PLL-RGD nanoparticles (DHAQ-NP), and evaluates antitumor efficacy of exercise and DHAQ-NP in hepatoma and breast carcinoma. The experimental findings demonstrate that DHAQ-NP group have more significant antitumor efficacy than DHAQ group in hepatoma-bearing mice and breast carcinoma-bearing mice. Compared with DHAQ-NP group, the antitumor efficacy of Exercise+DHAQ-NP group are significantly lower in breast carcinoma-bearing mice. However, the antitumor efficacy of Exercise+DHAQ-NP group have no significant change in hepatoma-bearing mice. This suggests that the same exercise intensity can cause different antitumor efficacies for different tumors undergoing targeted therapies. 相似文献
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通过含酪氨酸的聚磷酸酯与药物分子进行大分子反应,制备了含5-氟尿嘧啶或氨甲蝶呤的聚磷酸酯。所得聚磷酸酯均具有两亲性,部分聚磷酸酯在水中能形成胶束。研究了这些聚合物的体外降解和释药性能,体外抗肿瘤实验表明,有些聚磷酸酯药物具有较强的抗肿瘤活性。 相似文献
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氟尿嘧啶自旋标记衍生物的合成与抗肿瘤活性 总被引:2,自引:0,他引:2
稳定氮氧自由基作为某些抗癌药物的载体,不仅能提高药物对癌细胞的选择性,而且为借助电子自旋共振(ESR)技术研究药物的作用机理和代谢提供了一种新手段。在前文中,我们报道了几种5-氟尿嘧啶的自旋标记衍生物。作为这一工作的继续,本文报道一系列新的氟尿嘧啶自旋标记衍生物10_(a—c)、11_(a—c)和12_(a—c)的合成及其抗肿瘤活性的研究。 相似文献
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H Nowatari Y Kuroda H Hayami K Okamoto H Ekimoto K Takahashi 《Chemical & pharmaceutical bulletin》1989,37(9):2406-2409
Novel alkyl-1,4-butanediamine Pt(II) complexes having a seven-membered ring structure were synthesized and characterized by fast atom bombardment mass and infrared spectra and elemental analysis. Their antitumor activities in vivo toward lymphoid leukemia L1210 and Lewis lung carcinoma LL were studied in the case where the leaving group was either dichloride or cyclobutane-1,1-dicarboxylate. 1,4-Butanediamine Pt(II) complexes (seven-membered ring) showed higher antitumor activities than those of ethylenediamine Pt(II) (five-membered ring) and 1,3-propanediamine Pt(II) (six-membered ring) complexes toward L1210 for both leaving groups. Alkyl-1,4-butanediamine Pt(II) complexes showed high antitumor activities toward L1210, except for 1,1-dimethyl-1,4-butanediamine Pt(II) complexes. In particular, 2,2-dimethyl-1,4-butanediamine and 2,3-dimethyl-1,4-butanediamine Pt(II) complexes exhibited excellent antitumor activities with T/C% values higher than 300. None of the dichloro Pt(II) complexes showed antitumor activities toward LL, but the cyclobutane-1,1-dicarboxylato Pt(II) complexes, which were moderately active toward L1210 with T/C% values around 200, also showed high antitumor activities toward LL with T/C% values of more than 200. Alkyl-1,4-butanediamine Pt(II) complexes with a seven-membered ring structure were found to be stable and to have antitumor activities in vivo. 相似文献
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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 《中国化学快报》2014,25(7):978-982
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. 相似文献
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A new class of deoxyribonucleic acid (DNA)-intercalating antitumor agents, novel 9-anilino-2,3-ethylenedioxyacridines (five compounds) have been synthesized and evaluated for activity against P388 leukemia in vivo. A few of them possessed the same potency of antitumor activity as amsacrine (m-AMSA) which is an important antitumor agent in clinical use. 相似文献
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Matsuno T Karo M Sasahara H Watanabe T Inaba M Takahashi M Yaguchi SI Yoshioka K Sakato M Kawashima S 《Chemical & pharmaceutical bulletin》2000,48(11):1778-1781
Triamino-substituted 1,3,5-triazine and pyrimidine derivatives were synthesized and tested for antitumor activities using some human cancer cell lines and murine leukemia cell lines. All the compounds having benzimidazolyl and morpholino groups as substituents on the 1,3,5-triazine ring showed antitumor activity. Pyrimidine derivatives having the same groups as substituents also showed antitumor activity. Among them, the compounds having 1-benzimidazolyl, morpholino and cis-2,3-dimethylmorpholino groups as substituents on the 1,3,5-triazine ring or pyrimidine ring exhibited the most potent antitumor activity, and these compounds exhibited no or very weak aromatase inhibitory activity. In contrast, the compounds having imidazolyl group instead of benzimidazolyl group as a substituent on the 1,3,5-triazine ring showed a potent aromatase inhibitory activity. 相似文献
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Nian Guang Li Qi Dong You Xue Feng Huang Jin Xin Wang Qing Long Guo Xiao Guang Chen Yan Li Hong Yan Li Department of Medicinal Chemistry China Pharmaceutical University Nanjing China Department of Physiology China Pharmaceutical University Nanjing China Institute of Materia Medica Chinese Academy of Medical Science Peking Union Medical College Beijing China 《中国化学快报》2007,18(6):659-662
Through simplifying the complicated skeleton of the natural product gambogic acid, two series derivatives of chromone and xanthone were synthesized and examined for their antitumor activities against several cancer cells in vitro by MTT method. The results showed that appropriate introduction of prenyl group to the small molecular compounds could elevate their antitumor activities. The structure-activities relationship of synthesized compounds certified that the bridgecore in gambogic acid was very important for keeping its antitumor activities. 相似文献
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Zhen Yuan MIAO Wan Nian ZHANG Jian Zhong YAO Chun Quan SHENG Yun Long SONG Hui XU Min ZHANG Jing ZHANG 《中国化学快报》2006,17(6):720-722
Camptotecin is the parent of an important class of anticancer agents which, can selectively poison the ubiquitous nuclear enzyme topoisomerase. Water soluble camptothecin analogues such as topotecan and irinotecan are already approved for clinical uses in… 相似文献
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Synthesis and antitumor activity of novel 10-amino acids ester homocamptothecin analogues 总被引:2,自引:0,他引:2
Liang You Wan Nian Zhang Zhen Yuan Miao Wei Guo Xiao Ying Che Wen Ya Wang Chun Quan Sheng Jiang Zhong Yao Ting Zhou 《中国化学快报》2008,19(7):811-813
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 iritecan. 相似文献
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我国天然药物和中药资源丰富,种类繁多,可作为先导化合物进行修饰以提高可成药性。其中,黄酮类化合物是自然界中一种常见的天然多酚类化合物,在抗肿瘤方面具有其独特的生物活性;对其进行结构修饰与改造,可提高黄酮类化合物的生物利用度和抗肿瘤活性。本文通过查阅并整理近几年国内外的黄酮类化合物的相关文献,对黄酮类化合物的母核位点进行结构修饰与改造所得的101个黄酮类衍生物及其抗肿瘤活性及作用机制进行综述,同时讨论了构效关系,以期为黄酮类衍生物的结构修饰和抗肿瘤研究提供参考和帮助。 相似文献
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