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Keywords = phenylsulfonylurea

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13 pages, 2795 KiB  
Article
Design, Synthesis and Biological Evaluation of Novel Phenylsulfonylurea Derivatives as PI3K/mTOR Dual Inhibitors
by Bingbing Zhao, Fei Lei, Caolin Wang, Binliang Zhang, Zunhua Yang, Wei Li, Wufu Zhu and Shan Xu
Molecules 2018, 23(7), 1553; https://doi.org/10.3390/molecules23071553 - 27 Jun 2018
Cited by 13 | Viewed by 3773
Abstract
Five series of novel phenylsulfonylurea derivatives, 19ad, 20ad, 21ad, 22ad and 23ad, bearing 4-phenylaminoquinoline scaffold were designed, synthesized and their IC50 values against four cancer cell lines (HepG-2, [...] Read more.
Five series of novel phenylsulfonylurea derivatives, 19ad, 20ad, 21ad, 22ad and 23ad, bearing 4-phenylaminoquinoline scaffold were designed, synthesized and their IC50 values against four cancer cell lines (HepG-2, A549, PC-3 and MCF-7) were evaluated. Most compounds showed moderate cytotoxicity activity against the cancer cell lines. Structure–activity relationships (SARs) and pharmacological results indicated that introduction of 4-aminoquinoline scaffold and phenylsulfonylurea scaffold were beneficial for anti-tumor activity. Moreover, para-methoxyl substitution of 4-anilino moiety and para-halogen substitution of phenylsulfonylurea have different impacts on different series of compounds. Furthermore, the micromolecule group substitution in the 6-position of the quinoline ring have a slight impact on the cellular activity of the target compounds. Full article
(This article belongs to the Section Medicinal Chemistry)
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