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Your search keyword '"Wen, Zhongqing"' showing total 21 results
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21 results on '"Wen, Zhongqing"'

14. Syn-2, 3-diols and anti-inflammatory indole derivatives from Streptomyces sp. CB09001.

Author

Jiang, Lin, Pu, Hong, Qin, Xiangjing, Liu, Jianxin, Wen, Zhongqing, Huang, Yimin, Xiang, Jingxi, Xiang, Yunxi, Ju, Jianhua, Duan, Yanwen, and Huang, Yong

Subjects
INDOLE derivatives, STREPTOMYCES, NITRIC-oxide synthases, INDOLE, DITERPENES, THYMIDINE
Abstract

Two new natural diols, (2S, 3S, 4S)-4-methyl-1-phenylhexane-2,3-diol (1) and (2S, 3S)-4-methyl-1-phenylpentane-2,3-diol (2), together with five known compounds, xenocyloins B-D (3–5), lumichrome (6) and thymidine (7) were isolated from Streptomyces sp. CB09001. The absolute configurations of 1 and 2were established by crystallographic structure analysis. The anti-inflammatory effects of 1–7 were also investigated in RAW246.7 murine macrophage cells stimulated by lipopolysaccharide. The indole derivative xenocyloin B (3) significantly inhibited inducible nitric oxide synthase expression in RAW264.7 cells and could be a potential anti-inflammatory drug lead. [ABSTRACT FROM AUTHOR]

Published
2021
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15. Biomimetic Stereoselective Sulfa-Michael Addition Leads to Platensimycin and Platencin Sulfur Analogues against Methicillin-Resistant Staphylococcus aureus

Author

Qiu, Lin, Tian, Kai, Wen, Zhongqing, Deng, Youchao, Kang, Dingding, Liang, Haoyu, Zhu, Xiangcheng, Shen, Ben, Duan, Yanwen, and Huang, Yong

Abstract

Several sulfur-containing platensimycin (PTM) and platencin (PTN) analogues, with activities comparable to the parent natural products, have recently been discovered from microorganisms, implying a biomimetic route to diversify the PTM and PTN scaffolds for structure–activity relationship study. We present here a substrate-directed and scaleable semisynthetic strategy to make PTM and PTN sulfur analogues with excellent diasteroselectivity, without using any chiral catalysts. Most of the sulfur analogues showed strong activities against clinical Staphylococcus aureusisolates, with minimum inhibitory concentrations of 0.5–2 μg mL–1. Density functional theory calculations were in agreement with the observed selectivity for these analogues and suggest that the conformation restraints of the terpene cages of PTM and PTN on the transition states determine the si-face attack selectivity.

Published
2024
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18. Yangpumicins F and G, Enediyne Congeners from Micromonospora yangpuensisDSM 45577

Author

Wang, Zilong, Wen, Zhongqing, Liu, Ling, Zhu, Xiangcheng, Shen, Ben, Yan, Xiaohui, Duan, Yanwen, and Huang, Yong

Abstract

Enediyne natural products are among the most cytotoxic small molecules and thus excellent payload candidates for the development of antibody–drug conjugates (ADCs). Here we report the isolation and structural elucidation of two new 10-membered anthraquinone-fused enediynes, yangpumicins (YPM) F (6) and G (7), together with five known congeners, YPM A–E (1–5), from Micromonospora yangpuensisDSM 45577. YPM F (6) and G (7) showed strong cytotoxicity against the tested human cancer cell lines, as well as activity against several Gram-positive and Gram-negative pathogens. The 1,2-diols in 6and 7promise to enable new linker chemistry for the development of YPM-based ADCs.

Published
2019
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19. Semisynthesis of 3‐Hydroxyoxindole Rapamycin Analogues Through Site‐ and Stereoselective Trapping of Oxonium Ylides in RhII‐Catalyzed Three‐Component Reactions.

Author

Qiu, Lin, Su, Meng, Wen, Zhongqing, Zhu, Xiangcheng, Duan, Yanwen, and Huang, Yong

Subjects
YLIDES, TRAPPING, NATURAL products, RAPAMYCIN, ANTINEOPLASTIC agents
Abstract

The site‐ and diastereoselective functionalization of 40‐OH in rapamycin by 3‐hydroxyoxindole moieties was efficiently achieved through the active protic oxonium ylide trapping reactions using isatins, resulting in 31 new analogues of rapamycin. This study not only significantly expanded the known active rapalogs, but showcased the broad utility of multi‐component reactions in late‐stage functionalization of complex natural products. [ABSTRACT FROM AUTHOR]

Published
2019
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21. Discovery of a DNA Topoisomerase I Inhibitor Huanglongmycin N and Its Congeners from Streptomycessp. CB09001

Author

Zhu, Saibin, Wang, Yeji, Wen, Zhongqing, Duan, Yanwen, and Huang, Yong

Abstract

Huanglongmycin (HLM) congeners G–N (7–14) were isolated from Streptomycessp. CB09001. Among them, 10–12possesses a tricyclic scaffold with benzene-fused pyran/pyrone, confirmed by X-ray single crystal diffraction analysis of 12. The structure–activity relationship study of 1, 13, and 14revealed not only the stronger cytotoxicity of 14against tested cancer cells but also the critical role of the C-7 ethyl group of 14in its binding to the DNA–topoisomerase I complex.

Published
2021
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