Department of Pharmacy, Traditional Chinese Medical Hospital of Zhuji, Zhuji, Zhejiang, China.
Department of Gastroenterology, Traditional Chinese Medical Hospital of Zhuji, Zhuji, Zhejiang, China.
Arch Pharm (Weinheim). 2022 Sep;355(9):e2200106. doi: 10.1002/ardp.202200106. Epub 2022 May 9.
Leukemia, a hematological malignancy originating from the bone marrow, is the principal cancer of childhood. In recent decades, improved remission rates and survival of patients with leukemia have been achieved due to significant breakthroughs in the treatment. However, chemoresistance and relapse are common, creating an urgent need for the search for novel pharmaceutical interventions. 1,2,3-Triazole is one of the most fascinating pharmacophores in the discovery of new drugs, and several 1,2,3-triazole derivatives have already been used in clinics or are under clinical evaluation for the treatment of cancers. In particular, 1,2,3-triazole hybrids could suppress tumor proliferation, invasion, and metastasis by inhibiting enzymes, proteins, and receptors in cancer cells, revealing their potential as putative antileukemic agents. This review covers the recent advances regarding the 1,2,3-triazole hybrids with potential antileukemic activity, focusing on the chemical structures, structure-activity relationship, and mechanisms of action, covering articles published from January 2017 to January 2022.
白血病是一种起源于骨髓的血液系统恶性肿瘤,是儿童期的主要癌症。近几十年来,由于在治疗方面取得了重大突破,白血病患者的缓解率和生存率得到了提高。然而,化疗耐药和复发很常见,因此迫切需要寻找新的药物干预措施。1,2,3-三唑是新药发现中最引人注目的药效团之一,已有几种 1,2,3-三唑衍生物被用于临床或正在进行临床评估,以治疗癌症。特别是,1,2,3-三唑杂合体可以通过抑制癌细胞中的酶、蛋白质和受体来抑制肿瘤的增殖、侵袭和转移,显示出它们作为潜在的抗白血病药物的潜力。本文综述了具有潜在抗白血病活性的 1,2,3-三唑杂合体的最新进展,重点介绍了化学结构、构效关系和作用机制,涵盖了 2017 年 1 月至 2022 年 1 月发表的文章。