CSIR - Indian Institute of Chemical Technology, Division of Organic Chemistry, Tarnaka, Hyderabad, India.
Expert Opin Drug Discov. 2013 Mar;8(3):289-304. doi: 10.1517/17460441.2013.758630. Epub 2013 Jan 15.
Imidazothiazole derivatives have long been therapeutically used for the treatment of various diseases. In recent years, the imidazothiazole and chalcone moieties have emerged as important pharmacophores in the development of antitumor agents. Imidazothiazole-chalcone conjugates can be accessed by covalently binding these two powerful pharamacophore units. These conjugates are known to exhibit a wide range of biological properties, including anticancer, antimicrobial, anti-inflammatory and immunosuppressive activities. Their promising biological profile and easy synthetic accessibility have triggered investigations directed at the design and development of new imidazothiazole-chalcone conjugate derivatives as potential chemotherapeutics.
The present review focuses on recent reports of the syntheses and anticancer properties of various imidazothiazoles, chalcones and imidazothiazole-linked chalcone conjugates. Furthermore, the authors discuss the structure-activity relationships (SAR) of imidazothiazoles and chalcones and their conjugates as new antitumor agents, as well as in vitro and in vivo evaluation, clinical use and their future therapeutic applications.
A large number of imidazothiazoles, chalcones and a new series of imidazothiazole-chalcone conjugates possess potent anticancer activity that could be further developed as drug candidates. Imidazothiazole-based conjugates could also display synergistic effect, and still there is a need to use the drug combinations permitting lower dose and development of new generation of drugs. Despite encouraging observed results for their response to tumors in clinical studies, full characterization of their toxicity is further required for their clinical usage as safe drugs for the treatment of cancer.
咪唑并噻唑衍生物长期以来一直被用于治疗各种疾病。近年来，咪唑并噻唑和查耳酮部分已成为开发抗肿瘤药物的重要药效团。可以通过共价结合这两个强大的药效团单元来获得咪唑并噻唑-查耳酮缀合物。已知这些缀合物具有广泛的生物学特性，包括抗癌、抗菌、抗炎和免疫抑制活性。它们有希望的生物学特征和易于合成的可及性促使人们进行了设计和开发新的咪唑并噻唑-查耳酮缀合衍生物作为潜在化疗药物的研究。
本综述重点介绍了最近关于各种咪唑并噻唑、查耳酮和咪唑并噻唑连接的查耳酮缀合物的合成和抗癌特性的报道。此外，作者讨论了咪唑并噻唑和查耳酮及其缀合物作为新型抗肿瘤药物的构效关系（SAR），以及体外和体内评价、临床应用及其未来的治疗应用。
大量的咪唑并噻唑、查耳酮和一系列新的咪唑并噻唑-查耳酮缀合物具有很强的抗癌活性，可以进一步开发为候选药物。基于咪唑并噻唑的缀合物还可能显示协同作用，仍然需要使用允许降低剂量的药物组合和开发新一代药物。尽管在临床研究中观察到它们对肿瘤的反应令人鼓舞，但进一步需要对其毒性进行全面表征，以便将其作为治疗癌症的安全药物在临床上使用。
