M.M.College of Pharmacy, Maharishi Markandeshwar (Deemed to be) University, Mullana, Ambala, HR, India.
Mini Rev Med Chem. 2021;21(14):1849-1864. doi: 10.2174/1389557521666210225115055.
Styrylquinoline is a quinoline molecule linked to phenyl rings with an unsaturated ethylene linker, resulting in a flat and rigid conformation. The synthesis of the molecule was reported almost a century ago but was not much explored due to its adverse toxicity and poor selectivity. In the last two decades, a plethora of work was reported related to the synthesis and antiretroviral activity of several styrylquinoline derivatives. Later, other activities such as antimicrobial and anticancer abilities of these derivatives were also reported. In this review, we summarize the diverse steps of the development and analyze the spectrum of the activity of styrylquinolines and their utilization in drug design. Styrylquinolines are extensively explored for new pharmacological activities in recent years and this makes the moiety gain more visibility as a potential drug candidate and lead molecule in medicinal chemistry. The data obtained in vitro and ex vivo shed light on their different mechanism of action. Styrylquinoline has proved to be a potential lead molecule in medicinal chemist's toolkit due to the exploration of a variety of avenues of its activity as a drug candidate.
苯乙烯基喹啉是一种喹啉分子,与苯环通过不饱和乙烯键连接,形成平面刚性构象。该分子的合成在近一个世纪前就有报道,但由于其毒性大、选择性差,并未得到广泛研究。在过去的二十年中,大量有关几种苯乙烯基喹啉衍生物的合成和抗逆转录病毒活性的研究被报道。后来,人们还报道了这些衍生物的其他活性,如抗菌和抗癌能力。在这篇综述中,我们总结了其发展的各个阶段,并分析了苯乙烯基喹啉的活性谱及其在药物设计中的应用。近年来,人们广泛探索苯乙烯基喹啉的新药理活性,这使得该部分作为潜在药物候选物和药物化学中的先导分子获得了更多的关注。体外和体内获得的数据阐明了它们不同的作用机制。苯乙烯基喹啉已被证明是药物化学家工具包中的一个潜在的先导分子,因为人们探索了其作为药物候选物的多种活性途径。