Department of Studies in Chemistry, University of Mysore, Manasagangotri, Mysuru-570006, Karnataka, India.
Department of Studies in Organic Chemistry, University of Mysore, Manasagangotri, Mysuru-570006, Karnataka, India.
Curr Org Synth. 2020;17(3):243-250. doi: 10.2174/1570179417666200225123329.
Design of chemically novel, biologically potent small heterocyclic molecules with anticancer activities, which targets the enzyme heparanase has gained prominent clinical interest. We have synthesized a novel class of carboxamide derivatives by coupling various substituted aromatic acid hydrazides and triazoleamine with pyrrolidine carboxylic acid by using coupling agents. The synthesized compounds are characterized by spectroscopic techniques such as FT-IR, HRMS and NMR. These compounds are investigated for cytotoxicity on different cancer cell lines and heparanase inhibitory activity. Most of them showed moderate heparanase inhibitory activity and good cytotoxicity.
设计具有抗癌活性的新型化学、生物有效小分子，以肝素酶为靶点，已引起临床的关注。我们通过使用偶联剂，将各种取代的芳族酸酰肼和三唑胺与吡咯烷羧酸偶联，合成了一类新型的羧酰胺衍生物。通过傅里叶变换红外光谱（FT-IR）、高分辨质谱（HRMS）和核磁共振（NMR）等光谱技术对合成的化合物进行了表征。研究了这些化合物对不同癌细胞系的细胞毒性和肝素酶抑制活性。它们中的大多数表现出中等的肝素酶抑制活性和良好的细胞毒性。
