Pyrrolo[2,1-a]isoquinoline (PIq) is a nitrogen heterocyclic scaffold of diverse alkaloids endowed with several biological activities, including antiretroviral and antitumor activities. Several 5,6-dihydro-PIq (DHPIq) alkaloids, belonging to the lamellarins' family, have proved to be cytotoxic to tumor cells, as well as reversers of multidrug resistance. In this review, we provide an overview of the main achievements over the last decade in the synthetic approaches to access libraries of PIq compounds along with a survey, as comprehensive as possible, of bioactivity, mechanism of action, pharmacophore and structure-activity relationships of synthetic analogs of DHPIq-based alkaloids. The focus is mainly on the potential exploitation of the (DH)PIq scaffold in design and development of novel antitumor drugs.

中文翻译：

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吡咯并[2,1-a]异喹啉支架在药物开发中的应用：合成与药物化学研究的进展

吡咯并[2,1-a]异喹啉（PIq）是多种生物碱的氮杂环骨架，具有多种生物活性，包括抗逆转录病毒和抗肿瘤活性。几种属于薄片蛋白家族的5,6-二氢-PIq（DHPIq）生物碱已被证明对肿瘤细胞具有细胞毒性，并且具有多重耐药性的逆转作用。在这篇综述中，我们概述了过去十年来在PIq化合物库的合成方法中的主要成就，并尽可能全面地调查了生物活性，作用机理，药效基团和结构-活性之间的关系。 DHPIq基生物碱的合成类似物。重点主要放在（DH）PIq支架在新型抗肿瘤药物设计和开发中的潜在开发上。