- Pd-catalyzed C-S activation for [3 + 3] annulation of 2-(methylthio) benzofuran-3-carboxylates and 2-hydroxyphenylboronic acids: Synthesis of coumestan derivatives
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Pd-catalytic C-S activation was successfully applied to initiate the cross-coupling of (2-methylthio-3-ester)benzofurans with 2-hydroxyphenylboronic acids and sequential intramolecular transesterification process under Liebeskind-Srogl conditions. Thus, a novel [3 + 3] annulation strategy for efficient synthesis of coumestan derivatives has been developed from readily available starting materials.
- Liu, Jingxin,Liu, Yingjie,Du, Wenting,Dong, Ying,Liu, Jun,Wang, Mang
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Read Online
- Benzofuran-isatin conjugates as potent VEGFR-2 and cancer cell growth inhibitors
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A series of benzofuran-isatin conjugates 6a-l and 7a,b tethered by various alkyl linkers were synthesized and evaluated for their VEGFR-2 inhibitory activity and in vitro activity against a panel of cancer cell lines. Seven of them were comparable with or
- Zou, Yulin
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Read Online
- Design, synthesis and in vitro anti-bacterial activities of benzofuran-isatin hybrids
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A series of novel benzofuran-isatin hybrids 6a-x tethered through propylene, butylene, pentylene and hexylene were designed, synthesized and evaluated for their in vitro antibacterial activities against a panel of clinically important Gram-positive and Gr
- Wang, Yin-Ling,Zhao, Shi-Jia,Liu, Yi,Xu, Zhi
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p. 687 - 710
(2021/02/06)
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- A kind of benzofuran and benzofuran coumarin derivative and its preparation method and application (by machine translation)
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The invention discloses a formula (I), (II), (III), (IV) shown benzofurans and Coumestans derivative and its preparation method, and said styrene and furan and Coumestans derivative compound in the treatment of multi-drug resistant tuberculosis disease in the application. The invention surfactant and furan and Coumestans derivatives are a class of novel structure, the bacteriostatic effect is prominent anti-Mycobacterium tuberculosis compound, it is to Mycobacterium tuberculosis pks13 gene fragment encoding polyketide synthase as the acting target, inhibit the growth and reproduction of microorganisms, in particular inhibiting Mycobacterium tuberculosis in bacterial cell wall synthesis of branch, in the medical field has potential application prospect. (by machine translation)
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- Benzofuran-isatin-hydroxylimine/thiosemicarbazide hybrids: Design, synthesis and in vitro anti-mycobacterial activity evaluation
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A series of novel benzofuran-isatin-hydroxylimine/thiosemicarbazide hybrids were designed, synthesized and evaluated for their in vitro anti-TB activities against drug-sensitive MTB H37Rv and MDR-TB isolates as well as cytotoxicity. All benzofu
- Zhang, Yaohuan,Wang, Ruo,Zhang, Tesen,Yan, Weitao,Chen, Yihong,Zhang, Yanping,Zhou, Muyang
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p. 653 - 655
(2019/01/04)
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- Benzofuran–isatin Hybrids: Design, Synthesis, and In Vitro Anti-cancer Activities
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A series of novel benzofuran–isatin hybrids 6a–s tethered through propylene and butylene were designed, synthesized, and evaluated for their in vitro anti-cancer activities against HepG2 (liver carcinoma), Hela (cervical cancer), A549 (lung adenocarcinoma
- Diao, Quan-Ping,Guo, Hua,Wang, Gang-Qiang
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p. 1687 - 1693
(2019/04/08)
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- Design, synthesis and in vitro anti-bacterial activities of benzofuran-isatin hybrids
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A series of novel benzofuran-isatin hybrids 6a-x tethered through propylene, butylene, pentylene and hexylene were designed, synthesized and evaluated for their in vitro antibacterial activities against a panel of clinically important Gram-positive and Gr
- Wang, Yin-Ling,Zhao, Shi-Jia,Liu, Yi,Xu, Zhi
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p. 687 - 710
(2019/11/19)
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- Benzofuran-isatin-imine hybrids tethered via different length alkyl linkers: Design, synthesis and in vitro evaluation of anti-tubercular and anti-bacterial activities as well as cytotoxicity
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Herein we report the design and synthesis of twenty-two novel benzofuran-isatin-imine hybrids 7a-v tethered through propylene, butylene, pentylene and hexylene, and for the evaluation of their in vitro anti-tubercular and anti-bacterial activities as well
- Gao, Feng,Wang, Tengfei,Gao, Meixiang,Zhang, Xia,Liu, Zhuqing,Zhao, ShiJia,Lv, ZaoSheng,Xiao, Jiaqi
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p. 323 - 331
(2019/01/30)
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- Benzofuran-isatin hybrids tethered via different length alkyl linkers and their in vitro anti-mycobacterial activities
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A series of novel benzofuran-isatin hybrids 6a–m tethered through different length alkyl linkers propylene, butylene, pentylene and hexylene were designed, synthesized and evaluated for their in vitro anti-mycobacterial activities against both drug-suscep
- Gao, Feng,Chen, Zijian,Ma, Long,Qiu, Lin,Lin, Jianguo,Lu, Guangming
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p. 2652 - 2656
(2019/04/17)
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- Identification of Novel Coumestan Derivatives as Polyketide Synthase 13 Inhibitors against Mycobacterium tuberculosis
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Inhibition of the mycolic acid pathway has proven a viable strategy in antitubercular drug discovery. The AccA3/AccD4/FadD32/Pks13 complex of Mycobacterium tuberculosis constitutes an essential biosynthetic mechanism for mycolic acids. Small molecules targeting the thioesterase domain of Pks13 have been reported, including a benzofuran-based compound whose X-ray cocrystal structure has been very recently solved. Its initial inactivity in a serum inhibition titration (SIT) assay led us to further probe other structurally related benzofurans with the aim to improve their potency and bioavailability. Herein, we report our preliminary structure-activity relationship studies around this scaffold, highlighting a natural product-inspired cyclization strategy to form coumestans that are shown to be active in SIT. Whole genome deep sequencing of the coumestan-resistant mutants confirmed a single nucleotide polymorphism in the pks13 gene responsible for the resistance phenotype, demonstrating the druggability of this target for the development of new antitubercular agents.
- Zhang, Wei,Lun, Shichun,Wang, Shu-Huan,Jiang, Xing-Wu,Yang, Fan,Tang, Jie,Manson, Abigail L.,Earl, Ashlee M.,Gunosewoyo, Hendra,Bishai, William R.,Yu, Li-Fang
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p. 791 - 803
(2018/02/17)
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- INHIBITORS OF MECHANOTRANSDUCTION TO TREAT PAIN AND MODULATE TOUCH PERCEPTION
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The invention relates to chemical compounds that are useful as inhibitors of mechanotransduction in the treatment of pain and modulation of touch perception. The invention further relates to the topical administration of the compounds described herein in
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Page/Page column 41
(2018/06/30)
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- Design, synthesis, docking and anti-inflammatory evaluation of novel series of benzofuran based prodrugs
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Several new benzofuran derivatives were synthesized, via appropriate synthetic route as anti-inflammatory agents. The anti-inflammatory activity of the prepared compounds was evaluated using carrageenan rat model. Among the synthesized compounds, some compounds showed comparable anti-inflammatory activity to nimesulide, the standard drug taken for anti-inflammatory studies. Docking study of the prepared compounds was performed for the study of interaction of molecules with the active site of COX-2. Preliminary biological studies and docking gave an interesting insight, into the validity of employing benzofuran analogues as good anti-inflammatory agent.
- Yadav, Pratima,Singh, Praveen,Tewari, Ashish Kumar
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p. 2251 - 2255
(2014/05/20)
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- Mild and efficient synthesis of 3-acyl-5-hydroxybenzofurans via bismuth chloride-catalyzed cycloaddition of unactivated 1,4-benzoquinones with 1,3-dicarbonyl compounds
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A method to prepare a variety of substituted 3-acyl-5-hydroxybenzofurans efficiently that relies on bismuth chloride-catalyzed cycloaddition of unactivated 1,4-benzoquinones with 1,3-dicarbonyl compounds is reported. The reaction was shown to be operation
- Thirupathaiah,Venkateshwar Rao,Ramanna
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experimental part
p. 1521 - 1524
(2011/10/31)
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- Efficient synthesis of 3-acyl-5-hydroxybenzofurans via copper(II) triflate-catalyzed cycloaddition of unactivated 1,4-benzoquinones with 1,3-dicarbonyl compounds
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A method to prepare a variety of substituted 3-acyl-5-hydroxybenzofurans efficiently that relies on copper(II) triflate-catalyzed cycloaddition of unactivated 1,4-benzoquinones with 1,3-dicarbonyl compounds is reported. The reaction was shown to be operat
- Mothe, Srinivasa Reddy,Susanti, Dewi,Chan, Philip Wai Hong
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scheme or table
p. 2136 - 2140
(2010/05/19)
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