Medicinal and Process Chemistry Division, CSIR-Central Drug Research Institute Sector-10, Jankipuram Extension, Lucknow, 226031, India.
AcSIR-Academy of Scientific & Innovative Research (AcSIR), Ghaziabad, Uttar Pradesh, 201002, India.
ChemMedChem. 2023 Mar 1;18(5):e202200617. doi: 10.1002/cmdc.202200617. Epub 2023 Jan 16.
Benzoxazines and benzoxazepines are nitrogen and oxygen-containing six and seven-membered benzo-fused heterocyclic scaffolds, respectively. Benzoxazepines and benzoxazines are well-known pharmacophores in pharmaceutical chemistry, which are of significant interest and have been extensively studied because of their promising activity against various diseases including their wide range of anticancer activity. Several reports are known for synthesizing benzoxazine and benzoxazepine-based compounds in the literature. Herein this review provides a critical analysis of synthetic strategies towards benzoxazines and benzoxazepines along with various ranges of anticancer activities based on these molecules that have been reported from 2010 onwards. This review also focuses on the structure-activity relationship of the benzoxazine and benzoxazepine scaffolds containing bioactive compounds and describes how the structural modification affects their anticancer activity.
苯并恶嗪和苯并恶唑分别是含氮和含氧的六元和七元苯并稠合杂环支架。苯并恶唑和苯并恶嗪是药物化学中众所周知的药效团，由于它们对各种疾病（包括广泛的抗癌活性）具有有希望的活性，因此引起了广泛的关注并进行了广泛的研究。文献中已知有几种合成苯并恶嗪和苯并恶唑基化合物的方法。本文综述了 2010 年以来文献中报道的苯并恶嗪和苯并恶唑类化合物的合成策略以及基于这些分子的各种抗癌活性范围。本综述还重点介绍了含生物活性化合物的苯并恶嗪和苯并恶唑支架的结构-活性关系，并描述了结构修饰如何影响它们的抗癌活性。
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