新型吡唑-4-磺酰胺衍生物的抗增殖活性：合成与生物学评价
Antiproliferative Activity of New Pyrazole-4-sulfonamide Derivatives: Synthesis and Biological Evaluation.
作者信息
Mahesh Panasa, Akshinthala Parameswari, Katari Naresh Kumar, Gupta Lavleen Kumar, Panwar Dikshita, Sharma Manoj Kumar, Jonnalagadda Sreekantha Babu, Gundla Rambabu
机构信息
Department of Chemistry, GITAM Deemed to be University, Hyderabad, Telangana 502329, India.
Department of Science and Humanities, MLR Institute of Technology, Dundigal, Medchal, Hyderabad, Telangana 500 043, India.
出版信息
ACS Omega. 2023 Jul 13;8(29):25698-25709. doi: 10.1021/acsomega.2c07539. eCollection 2023 Jul 25.
Pyrazole and sulfonamide constitute an important class of drugs, with several types of pharmacological agents. Facile synthesis of two new series of 3,5-dimethyl-1-pyrazole-4-sulfonamide and 1,3,5-trimethyl-1-pyrazole-4-sulfonamide derivatives was designed and synthesized. These pyrazole-4-sulfonamide derivatives are characterized by Fourier transform infrared (FT-IR), H NMR, C NMR, and elemental analysis, and their biological evolution data are presented. This paved way for the development of new pyrazole-4-sulfonamide derivatives. These compounds are tested for their in vitro antiproliferative activity against U937 cells by the CellTiter-Glo Luminescent cell viability assay using Mitomycin C. Cytotoxicity detection is based on the measurement of LDH activity, while these compounds did not exhibit cytotoxic activity on these cells. Half maximal inhibitory concentration (IC) was calculated by Graph Pad Prism software for each dose. Their structure-activity relationships were obtained and discussed.
吡唑和磺酰胺构成了一类重要的药物，有多种类型的药理剂。设计并合成了两个新系列的3,5-二甲基-1-吡唑-4-磺酰胺和1,3,5-三甲基-1-吡唑-4-磺酰胺衍生物。这些吡唑-4-磺酰胺衍生物通过傅里叶变换红外光谱（FT-IR）、氢核磁共振（¹H NMR）、碳核磁共振（¹³C NMR）和元素分析进行表征，并给出了它们的生物学活性数据。这为新型吡唑-4-磺酰胺衍生物的开发铺平了道路。通过使用丝裂霉素C的CellTiter-Glo发光细胞活力测定法，对这些化合物针对U937细胞的体外抗增殖活性进行了测试。细胞毒性检测基于乳酸脱氢酶（LDH）活性的测量，而这些化合物在这些细胞上未表现出细胞毒性活性。使用Graph Pad Prism软件为每个剂量计算半数最大抑制浓度（IC₅₀）。获得并讨论了它们的构效关系。
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