Design, synthesis and biological evaluation of novel macrocyclic bisbibenzyl analogues as tubulin polymerization inhibitors

Sun, Bin; Li, Lin; Hu, Qingwen; Xie, Fei; Zheng, Hongbo; Niu, Huanmin; Yuan, Huipin; Lou, Hongxiang

doi:10.1016/j.ejmech.2016.06.007

Cited by 12 publications

(3 citation statements)

References 37 publications

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“…The antiproliferative activity of these marchantin C analogues revealed that the most potent compounds 40 and 41 (Figure ) showed outstanding antiproliferative effects toward four kinds of cancer cell lines (i.e., HeLa, HT29, k562, and HCC1428), which was significantly superior to that of marchantin C. More importantly, compounds 40 and 41 could effectively inhibit the growth of the paclitaxel-resistant PC-3/Doc cancer cell line. Further biochemistry experiments demonstrated that these two compounds possessed excellent inhibition against tubulin polymerization in the tested HCC1482 cells and could abort the cell cycle of HCC1482 cells at the G2/M phase. , The above-mentioned natural product analogues 39 , 40 , and 41 with the DE scaffold provide several new and promising candidates for the development of novel antitumor agents targeting tubulin.…”

Section: Application Of De Scaffold In Medicinal Chemistrymentioning

confidence: 90%

“…Further biochemistry experiments demonstrated that these two compounds possessed excellent inhibition against tubulin polymerization in the tested HCC1482 cells and could abort the cell cycle of HCC1482 cells at the G2/M phase. 57,58 The above-mentioned natural product analogues 39, 40, and 41 with the DE scaffold provide several new and promising candidates for the development of novel antitumor agents targeting tubulin.…”

Section: ■ Introductionmentioning

confidence: 99%

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Diaryl Ether: A Privileged Scaffold for Drug and Agrochemical Discovery

Chen

Xiong

Yang

et al. 2020

J. Agric. Food Chem.

100

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Diaryl ether (DE) is a functional scaffold existing widely both in natural products (NPs) and synthetic organic compounds. Statistically, DE is the second most popular and enduring scaffold within the numerous medicinal chemistry and agrochemical reports. Given its unique physicochemical properties and potential biological activities, DE nucleus is recognized as a fundamental element of medicinal and agrochemical agents aimed at different biological targets. Its drug-like derivatives have been extensively synthesized with interesting biological features including anticancer, anti-inflammatory, antiviral, antibacterial, antimalarial, herbicidal, fungicidal, insecticidal, and so on. In this review, we highlight the medicinal and agrochemical versatility of the DE motif according to the published information in the past decade and comprehensively give a summary of the target recognition, structure–activity relationship (SAR), and mechanism of action of its analogues. It is expected that this profile may provide valuable guidance for the discovery of new active ingredients both in drug and pesticide research.

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Section: Application Of De Scaffold In Medicinal Chemistrymentioning

confidence: 90%

Section: ■ Introductionmentioning

confidence: 99%

Diaryl Ether: A Privileged Scaffold for Drug and Agrochemical Discovery

Chen

Xiong

Yang

et al. 2020

J. Agric. Food Chem.

100

View full text Add to dashboard Cite

show abstract

“…Even though, many drugs could be brominated under mild oxidation reagent DMSO and relatively low temperature ( Scheme 10 a) 157 . Lou group used this strategy to brominate Marchantin C, and obtained a series of analogs with anticancer activity 2–6 fold higher 158 . In 2022, Jiao and coworkers made a breakthrough in bromination of electron-deficient aromatic rings.…”

Section: Halogenation Of Bioactive Compoundsmentioning

confidence: 99%