Abstract A series of novel N‐thiadiazolylbenzisoselenazolone derivatives (VI) (I5 examples) is synthesized and evaluated for in vitro antiproliferative activity against 3 different human tumor cell lines.

10.1002/chin.201240204

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Design, synthesis and biological evaluation of buthutin derivatives as cardioprotective agents

Natural Products and Bioprospecting (2025)

Yuan Liu Fa-Qi Wang Xiaoyang Hua Shuhan Yang Li‐Ning Wang

Abstract Natural products are the important sources in cardiovascular drug development. In this study, twenty-nine buthutin derivatives were designed, synthesized, and evaluated for their NHE-1 inhibition and protective effects on cardiomyocyte injury. The structure of the newly synthesized compounds had been confirmed by 1 H-NMR, 13 C-NMR, and HR-ESI-MS spectra. Among all target compounds at 1 μM, compounds 9d , 9f , 9k , 9m , and 9n , with a protection ratio exceeding 30%, exerted stronger protective effects on H9c2 cardiomyocyte than positive control dexrazoxane and buthutin A. Meanwhile, compounds 9k , 9m , and 9o showed the significant NHE-1 inhibitory activities on H9c2 cardiomyocyte, all with a dpHi/min value less than 0.23. What is more, compounds 9k , 9m , 9o and buthutin A all exhibited the specificity on NHE-1 inhibition. Molecular modelling studies suggested the ability of compounds 9m and 9o to establish interactions with three hydrogen bonds to Asp267 and Glu346 of NHE-1, but also the ability with much lower CDOCKER energies than positive control cariporide and buthutin A. The structure–activity relationship (SAR) studies suggested that the presences of amide group, four-carbon linker, and para hydroxyl benzene ring were advantageous pharmacophores for above two pharmacological actions. This research would open new avenues for developing amide-guanidine-based cardioprotective agents. Graphical Abstract

Amide

Guanidine

Proton NMR

Bioorganic chemistry

10.1007/s13659-025-00497-9

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Synthesis and in vitro antiproliferative evaluation of novel nonsymmetrical disulfides bearing 1,3,4-oxadiazole moiety

Bioorganic & Medicinal Chemistry Letters (2016)

Jijun Zhao Xuefeng Wang Baolin Li Rui-Lian Zhang Bo Li

HeLa

Moiety

IC50

Oxadiazole

10.1016/j.bmcl.2016.08.014

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ChemInform Abstract: New Phenolic Compounds from the Seeds of Nigella glandulifera and Their Inhibitory Activities Against Human Cancer Cells.

ChemInform (2015)

Lu Sun Yu‐Ming Liu Bao‐Quan Chen Qinghua Liu

Abstract Three new phenolic compounds (I), (II), and (III) are isolated from the seeds of Nigella glandulifera together with a known compound.

10.1002/chin.201601203

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Synthesis, Characterization and Anti-hepatoma Activity of New Hederagenin Derivatives

Mini-Reviews in Medicinal Chemistry (2020)

Xiao Liu Lu Sun Qinghua Liu Baoquan Chen Yu‐Ming Liu

Based on the biological significance of hederagenin-type saponins found in our previous investigation, a series of new hederagenin derivatives were designed and synthesized.Their in vitro antiproliferative activities were evaluated against the HepG2 liver cancer cell line and normal cell line L929 by MTT assay.The preliminary bioassay results demonstrated that all the tested compounds 1-7 showed potent anti-hepatoma activities, and some compounds exhibited better effects than 5-fluorouracil against human hepatocellular carcinoma HepG2 cell line. Furthermore, compound 5 showed a significant antihepatoma activity against HepG2 cells with an IC50 value of 1.88 µM. Besides, all of the tested compounds showed a low cytotoxic effect against the normal cell line L929.All the compounds 1-7 displayed superior selectivity against human hepatocellular carcinoma HepG2 cell line, and the results suggest that the structural modifications of C ring on the hederagenin backbone are vital for modulating anti-hepatoma activities.

Hederagenin

IC50

Hep G2

Cancer cell lines

MTT assay

Hepatic carcinoma

10.2174/1389557519666191010091612

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Citations (3)