Kumar Sumit, Saha Sourav Taru, Gu Liang, Palma Gabriella, Perumal Shanen, Singh-Pillay Ashona, Singh Parvesh, Anand Amit, Kaur Mandeep, Kumar Vipan
Department of Chemistry, Guru Nanak Dev University, Amritsar 143005, India.
School of Molecular and Cell Biology, University of the Witwatersrand, Private Bag 3, Wits, 2050 Johannesburg, South Africa.
ACS Omega. 2018 Sep 30;3(9):12106-12113. doi: 10.1021/acsomega.8b01513. Epub 2018 Sep 27.
1-1,2,3-Triazole tethered imidazole-isatin and imidazole-isatin-thiosemicarbazone conjugates were synthesized and evaluated against MCF-7 and MDA-MB-231 cell lines. Antiproliferative activities of the synthesized conjugates revealed an optimum combination of longer alkyl chain length as spacer and a halogen-substituent on the isatin ring as a pre-requisite for good activity. The compound with an optimum combination of chloro-substituent at C-5 position of isatin ring and a butyl chain length proved to be most active and noncytotoxic with IC of 54.25 and 26.12 μM against MCF-7 and MDA-MB-231 cell lines, respectively.
合成了1,2,3-三唑连接的咪唑-异吲哚酮和咪唑-异吲哚酮-硫代半卡巴腙共轭物,并针对MCF-7和MDA-MB-231细胞系进行了评估。合成共轭物的抗增殖活性表明,较长的烷基链长度作为间隔基以及异吲哚酮环上的卤素取代基的最佳组合是良好活性的先决条件。异吲哚酮环C-5位氯取代基和丁基链长度的最佳组合的化合物被证明活性最高且无细胞毒性,对MCF-7和MDA-MB-231细胞系的IC分别为54.25和26.12 μM。