Abstract
Primary arylsulfonamide functional groups feature prominently in diverse pharmaceuticals. However, natural arylsulfonamides are relatively infrequent. In this work, two novel arylsulfonamide natural products were first synthesized, and then a series of novel molecules derived from natural arylsulfonamides were designed and synthesized, and their in vitro cytotoxic activities against A875, HepG2, and MARC145 cell lines were systematically evaluated. The results indicate that some of these arylsulfonamide derivatives exhibit significantly good cytotoxic activity against the tested cell lines compared with the control 5-fluorouracil (5-FU), such as compounds 10l, 10p, 10q, and 10r. In particular, the potential molecule 10q, containing a carbazole moiety, exhibited the highest inhibitory activity against all tested cell lines, with IC50 values of 4.19 ± 0.78, 3.55 ± 0.63, and 2.95 ± 0.78 μg/mL, respectively. This will offer the potential to discover novel drug-like compounds from the sparsely populated area of natural products that can lead to effective anticancer agents.
Highlights
From the roots and rhizomes of Tupistra chinensis Baker [20], whereas the result of in vitro cytotoxic activity in the human cancer cell lines indicated that the novel arylsulfonamide natural products displayed weak cytotoxicity
Based on the preliminary screening results, we found that some of these arylsulfonamide derivatives indicated moderate-to-good inhibition activity against all tested cell lines
The compounds 10l, 10p, 10q, and 10r exhibited significantly higher activities compared with the control at a concentration of 40 μg/mL (Figure 4), demonstrating that these natural-product-inspired molecules derived from sargassulfamide A could be considered as promising scaffolds for developing effective anticancer agents
Summary
Natural products (NPs) and their molecular scaffolds have a long tradition of offering chemists a range of uncharted chemotypes as valuable starting points for the development of novel drugs [1,2,3], and have been a major source of anticancer drug discovery [4,5,6,7]. Sargassulfamide A, bearing a rare and unique sulfonamide group, was isolated from the seaweed Sargassum naozhouense [19] Almost simultaneously, another novel arylsulfonamide natural product was isolated together with sargassulfamide A from the roots and rhizomes of Tupistra chinensis Baker [20], whereas the result of in vitro cytotoxic activity in the human cancer cell lines indicated that the novel arylsulfonamide natural products displayed weak cytotoxicity. Structural tial bioactivity of some natural compounds has been seriously limited. 2. Design strategy of natural arylsulfonamide-inspired molecules. Molecules 2022, 27, x FOR PEER REVIEW as shown in Scheme 1, and their cytotoxic activities against several human cancer cell lines—including A875, HepG2, and MARC145—were systematically evaluated by the colorimetric method for the time.time.
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