Abstract:
The search for better chemotherapeutic drugs to alleviate the deficiencies of existing platinum (Pt) drugs has picked up the pace in the millennium. There has been a disparate effort to design better and safer Pt drugs to deal with the problems of deactivation, Pt resistance and toxic side effects of clinical Pt drugs. In this review, we have discussed the potential of kinetically inert Pt complexes as an emerging class of next-generation Pt drugs. The introduction gives an overview about the development, use, mechanism of action and side effects of clinical Pt drugs as well as the various approaches to improve some of their pharmacological properties. We then describe the impact of kinetic lability on the pharmacology of functional Pt drugs including deactivation, antitumor efficacy, toxicity and resistance. Following a brief overview of numerous pharmacological advantages that a non-functional kinetically inert Pt complex can offer; we discussed structurally different classes of kinetically inert Pt (II) complexes highlighting their unique pharmacological features.
摘要:
寻求更好的化疗药物以减轻现有铂(Pt)药物的缺陷在千年中加快了步伐。有一个不同的努力,设计更好,更安全的铂药物来处理失活的问题,临床铂类药物的铂耐药性及毒副作用。在这次审查中,我们已经讨论了动力学惰性Pt配合物作为新一代Pt药物的潜力。引言概述了发展,使用,的作用机制和临床铂药物的副作用,以及各种方法,以改善其一些药理性质。然后,我们描述了动力学不稳定性对功能性Pt药物的药理学的影响,包括失活,抗肿瘤疗效,毒性和抗性。在简要概述了非功能性动力学惰性Pt络合物可以提供的许多药理学优势之后;我们讨论了结构上不同类别的动力学惰性Pt(II)络合物,突出了它们独特的药理学特征。