Lobe Maloba M M, Efange Simon M N
Department of Chemistry, University of Buea, PO Box 63, Buea, Cameroon.
R Soc Open Sci. 2020 Jan 8;7(1):191316. doi: 10.1098/rsos.191316. eCollection 2020 Jan.
Both tetrahydroisoquinolines (THIQs) and oxindoles (OXs) display a broad range of biological activities including anti-cancer activity, and are therefore recognized as two privileged scaffolds in drug discovery. In the present study, 24 3',4'-dihydro-2'H-spiro[indoline-3,1'-isoquinolin]-2-ones, designed as molecular hybrids of THIQ and OX, were synthesized and screened against 59 cell lines in the NCI-60 screen. Twenty compounds displayed weak to moderate inhibition of cell proliferation; among them, three compounds displayed at least 50% inhibition of cell proliferation. The compounds appeared to target primarily renal cell cancer lines; however, leukaemia, melanoma, non-small cell lung cancer, prostate, ovarian and even breast cancer cell lines were also affected. Therefore, this class of spirooxindoles may provide useful leads in the search for new anti-cancer agents.
四氢异喹啉（THIQs）和氧化吲哚（OXs）均具有广泛的生物活性，包括抗癌活性，因此被认为是药物研发中两类具有优势的骨架结构。在本研究中，设计合成了24种作为THIQ和OX分子杂合体的3'，4'-二氢-2'H-螺[吲哚啉-3,1'-异喹啉]-2-酮，并在NCI-60筛选中针对59种细胞系进行了筛选。20种化合物表现出对细胞增殖的弱至中度抑制作用；其中，三种化合物对细胞增殖的抑制率至少达到50%。这些化合物似乎主要靶向肾癌细胞系；然而，白血病、黑色素瘤、非小细胞肺癌、前列腺癌、卵巢癌甚至乳腺癌细胞系也受到了影响。因此，这类螺环氧化吲哚可能为寻找新型抗癌药物提供有用的先导化合物。
