Cancer is one of the diseases with high morbidity and mortality on a global scale. Chemotherapy remains the primary treatment option for most cancer patients, including patients with progressive, metastatic, and recurrent diseases. To date, hundreds of chemotherapy drugs are used to treat various cancers, however, the anti-cancer efficacy and outcomes are largely hampered by chemotherapy-associated toxicity and acquired therapeutic resistance. The natural product (NP) oridonin has been extensively studied for its anti-cancer efficacy. More recently, oridonin has been shown to overcome drug resistance through multiple mechanisms, with yet-to-be-defined bona fide targets. Hundreds of oridonin derivative analogs (oridonalogs) have been synthesized and screened for improved potency, bioavailability, and other drug properties. Particularly, many of these oridonalogs have been tested against oridonin for tumor growth inhibition, potential for overcoming therapeutic resistance, and immunity modulation. This concise review seeks to summarize the advances in this field in light of identifying clinical-trial level drug candidates with the promise for treating progressive cancers and reversing chemoresistance.

癌症是全球范围内发病率和死亡率都很高的疾病之一。化疗仍然是大多数癌症患者的主要治疗选择，包括患有进行性、转移性和复发性疾病的患者。迄今为止，数百种化疗药物被用于治疗各种癌症，然而，抗癌功效和结果在很大程度上受到化疗相关毒性和获得性治疗耐药性的阻碍。天然产物 (NP) oridonin 的抗癌功效已被广泛研究。最近，冬凌草胺已被证明可以通过多种机制克服耐药性，但真正的尚未确定目标。数百种冬凌草素衍生物类似物（冬凌草胺类似物）已被合成和筛选，以提高效力、生物利用度和其他药物特性。特别是，许多这些 oridonalogs 已针对 oridonin 进行了肿瘤生长抑制、克服治疗抗性和免疫调节的潜力的测试。这篇简明的综述旨在总结该领域的进展，以确定临床试验水平的候选药物，这些候选药物有望治疗进行性癌症和逆转化学耐药性。