5010-38-8Relevant academic research and scientific papers
Design, Synthesis, and In Vitro Anti-mycobacterial Activities of Propylene Tethered Benzofuran–Isatin Hybrids
Guo, Hua
, p. 338 - 342 (2019)
A series of novel propylene tethered benzofuran–isatin hybrids 5a–j were designed, synthesized, and assessed for their in vitro anti-mycobacterial activity against Mycobacterium tuberculosis (MTB) H37Rv and multidrug-resistant (MDR)-MTB strains
Design, synthesis and in vitro anti-bacterial activities of benzofuran-isatin hybrids
Wang, Yin-Ling,Zhao, Shi-Jia,Liu, Yi,Xu, Zhi
, p. 687 - 710 (2021/02/06)
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
Benzofuran-isatin conjugates as potent VEGFR-2 and cancer cell growth inhibitors
Zou, Yulin
, p. 510 - 516 (2019/11/19)
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
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
Gao, Feng,Wang, Tengfei,Gao, Meixiang,Zhang, Xia,Liu, Zhuqing,Zhao, ShiJia,Lv, ZaoSheng,Xiao, Jiaqi
, p. 323 - 331 (2019/01/30)
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
Benzofuran-isatin hybrids tethered via different length alkyl linkers and their in vitro anti-mycobacterial activities
Gao, Feng,Chen, Zijian,Ma, Long,Qiu, Lin,Lin, Jianguo,Lu, Guangming
, p. 2652 - 2656 (2019/04/17)
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
Benzofuran-isatin-hydroxylimine/thiosemicarbazide hybrids: Design, synthesis and in vitro anti-mycobacterial activity evaluation
Zhang, Yaohuan,Wang, Ruo,Zhang, Tesen,Yan, Weitao,Chen, Yihong,Zhang, Yanping,Zhou, Muyang
, p. 653 - 655 (2019/01/04)
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
Benzofuran–isatin Hybrids: Design, Synthesis, and In Vitro Anti-cancer Activities
Diao, Quan-Ping,Guo, Hua,Wang, Gang-Qiang
, p. 1687 - 1693 (2019/04/08)
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
Design, synthesis and in vitro anti-bacterial activities of benzofuran-isatin hybrids
Wang, Yin-Ling,Zhao, Shi-Jia,Liu, Yi,Xu, Zhi
, p. 687 - 710 (2019/11/19)
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
Identification of Novel Coumestan Derivatives as Polyketide Synthase 13 Inhibitors against Mycobacterium tuberculosis
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
, p. 791 - 803 (2018/02/17)
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.
Design, synthesis and anti-mycobacterial activity evaluation of benzofuran-isatin hybrids
Gao, Feng,Yang, Hua,Lu, Tianyu,Chen, Zijian,Ma, Long,Xu, Zhi,Schaffer, Paul,Lu, Guangming
, p. 277 - 281 (2018/10/15)
Herein we report the design and synthesis of a series of novel benzofuran-isatin hybrids, and in vitro evaluation of their anti-mycobacterial activity against both drug-susceptible and multi-drug resistant (MDR) Mycobacterium tuberculosis (MTB) strains. I
