Cancer is one of the leading groups of threatened caused by abnormal state cell growth and second leading diseases involved in the major global death. To treat this, research looking for promising anticancer drugs from natural resource, or synthesized novel molecules by diverse group of scientists worldwide. Currently, drugs get into clinical practices and showing side effects with target actions which in turn leading to multidrug resistance unknowingly. Podophyllotoxin, a naturally occurring lignan and with hybrids have become one of the most attractive subjects due to their broad spectrum of pharmacological activities. Podophyllotoxin derivatives have been the centre of attention of extensive chemical amendment and pharmacological investigation in modern decades. Mainly, the innovation of the semi-synthetic anticancer drugs etoposide and teniposide has stimulated prolonged research interest in this structural phenotype. The present review focuses mainly on new anticancer drugs from podophyllotoxin analogs, mechanism of action and their structure–activity relationships (SAR) as potential anticancer candidates for future discovery of suitable drug candidates.

癌症是由异常状态细胞生长和与全球主要死亡相关的第二大主要疾病造成的威胁的主要类别之一。为了解决这个问题，全球范围内的科学家们从自然资源中寻找有前途的抗癌药物或合成的新型分子的研究。当前，药物进入临床实践并以靶标作用表现出副作用，这又在不知不觉中导致多药耐药性。鬼臼毒素，一种天然存在的木脂素，与杂种混合，由于其广泛的药理活性而已成为最吸引人的主题之一。鬼臼毒素衍生物已成为近几十年来广泛的化学修饰和药理研究的焦点。主要是 半合成抗癌药依托泊苷和替尼泊苷的创新激发了对该结构表型的长期研究兴趣。本综述主要集中于鬼臼毒素类似物的新抗癌药物，作用机制及其结构-活性关系（SAR），它们是潜在的候选抗癌药物，可用于未来发现合适的候选药物。