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Oxadiazoles as privileged motifs for promising anticancer leads: Recent advances and future prospects

机译:恶二唑作为有前景的抗癌药物的优先基序:最新进展和未来前景

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摘要

Taking into account the rising trend of the incidence of cancers of various organs, effective therapies are urgently needed to control human malignancies. The rapid emergence of hundreds of new agents that modulate an ever-growing list of cancer-specific molecular targets offers tremendous hope for cancer patients. However, almost all of the chemotherapy drugs currently on the market cause serious side effects. Based on these facts, the design of new chemical entities as anticancer agents requires the simulation of a suitable bioactive pharmacophore. The pharmacophore not only should have the required potency but must also be safer on normal cell lines than on tumor cells. In this perspective, oxadiazole scaffolds with well-defined anticancer activity profile have fueled intense academic and industrial research in recent years. This paper is intended to highlight the recent advances along with current developments as well as future outlooks for the design of novel and efficacious anticancer agents based on oxadiazole motifs. The search for biologically promising, new chemical entities against the deadly cancer disease remains an important theme in drug discovery. Although many drug molecules are already in use for the treatment of cancer, there are still a lot of challenges in the development of new drug candidates. This paper surveys the recent efforts undertaken for the identification, optimization, and development of potent anticancer agents.
机译:考虑到各种器官的癌症发生率的上升趋势,迫切需要有效的疗法来控制人类恶性肿瘤。数百种新试剂的出现迅速改变了癌症特定分子靶标的清单,为癌症患者带来了巨大希望。但是,目前市场上几乎所有的化学治疗药物都会引起严重的副作用。基于这些事实,设计新的化学实体作为抗癌剂需要模拟合适的生物活性药效团。该药效团不仅应具有所需的效力,而且在正常细胞系上也必须比在肿瘤细胞上更安全。从这个角度来看,近年来,具有明确抗癌活性的恶二唑支架助长了学术和工业研究的热情。本文旨在突出基于恶二唑基序的新型,有效抗癌剂设计的最新进展以及当前的发展以及对未来的展望。寻找具有生物学前途的新化学实体以对抗致命的癌症疾病仍然是药物发现中的重要主题。尽管许多药物分子已经用于治疗癌症,但是在开发新药物候选药物方面仍然存在许多挑战。本文概述了为鉴定,优化和开发有效的抗癌药物所做的最新努力。

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