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Feng Y.,Zhejiang Xianju Pharmaceutical | Ying L.,Zhejiang Silver Elephant Bio Engineering Co. | Zhang C.,Zhejiang University
Acta Crystallographica Section E: Structure Reports Online | Year: 2010

In the title compound, C15H14O3S, the dihedral angle between the two benzene rings is 59.3 (8)°. The crystal structure is stabilized by weak intermolecular C - H⋯π interactions between the benzene rings and the central ethyl-ene bridge, and a weak non-classical C - H⋯O hydrogen bond occurs in the structure. © 2010.


Lv K.,Chinese Academy of Sciences | Sun Y.,Chinese Academy of Sciences | Sun L.,Chinese Academy of Sciences | Wei Z.,Chinese Academy of Sciences | And 3 more authors.
ChemMedChem | Year: 2012

A series of novel (R)/(S)-7-(3-alkoxyimino-2-aminomethyl-1-azetidinyl)fluoroquinolone derivatives were synthesized and evaluated for their invitro antibacterial activity against representative strains. Our results reveal that 12 of the target compounds generally show better activity (MIC: <0.008-0.5μgmL -1) against the tested Gram-positive strains including MRSA and MRSE than levofloxacin (LVFX, MIC: 0.125-8μgmL -1). Their activity is similar to that of gemifloxacin (GMFX, MIC: <0.008-4μgmL -1). However, they are generally less active than the two reference drugs against Gram-negative strains. Moreover, against clinical strains of S.aureus including MRSA and S.epidermidis including MRSE, the MIC 50 values (0.06-16μgmL -1) and MIC 90 values (0.5-32μgmL -1) of compounds 16w, y, and z are 2-8- and 2-16-fold less than LVFX, respectively, and 16w (MIC 90 range: 0.5-4μgmL -1) was also found to be more active than GMFX (MIC 90 range: 1-8μgmL -1). © 2012 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.


Lv K.,Peking Union Medical College | Wu J.,Zhejiang Xianju Pharmaceutical | Wang J.,No 5 Hospital Of Harbin | Liu M.,Peking Union Medical College | And 4 more authors.
Bioorganic and Medicinal Chemistry Letters | Year: 2013

We report herein the synthesis of a series of 7-[3-alkoxyimino-4-(methyl) aminopiperidin-1-yl]quinolone/naphthyridone derivatives. In vitro antibacterial activity of these derivatives was evaluated against representative strains, and compared with ciprofloxacin (CPFX), levofloxacin (LVFX) and gemifloxacin (GMFX). The results reveal that all of the target compounds 19a-c and 20 have considerable Gram-positive activity, although they are generally less active than the reference drugs against the Gram-negative strains with some exceptions. Especially, novel compounds 19a2, 19a4 and 19a5 were found to show strong antibacterial activity (MICs: <0.008-0.5 μg/mL) against all of the tested 15 Gram-positive strains including MRSA, LVFX- and GMFX-resistant MRSE, and CPFX-, LVFX- and GMFX-resistant MSSA. © 2013 Elsevier Ltd. All rights reserved.


Huang Y.,Fudan University | Liu M.,Fudan University | Meng L.,Fudan University | Feng P.,Fudan University | And 4 more authors.
Steroids | Year: 2015

Abstract Thirteen novel furoxan-based nitric oxide (NO) releasing hybrids (14a-e, 15a-e, 17b-d) of 16,17-pyrazo-annulated steroidal derivatives were synthesized and evaluated against the MDA-MB-231, HCC1806, SKOV-3, DU145, and HUVEC cell lines for their in vitro anti-proliferative activity. Most of the compounds displayed potent anti-proliferative effects. Among them, 17c exhibited the best activity with IC50 values of 20-1.4 nM against four cell lines (MDA-MB-231, SKOV-3, DU145, and HUVEC), and 1.03 μM against a tamoxifen resistant breast cancer cell line (HCC1806). Furthermore, five compounds (14a, 15a, 17b-d) were selected to screen for VEGF inhibitory activity. Compounds 15a, 17b,c showed obviously better activity than 2-Methoxyestradiol (2-ME) on reducing levels of VEGF secreted by MDA-MB-231 cell line. In a Capillary-like Tube Formation Assay, compounds 17b,c exhibited a significant suppression of the tubule formation in the concentration of 1.75 nM and 58 nM, respectively. The preliminary SAR showed that steroidal scaffolds with a linker in 3-position were favorable moieties to evidently increase the bioactivities of these hybrids. Overall, these results implied that 17c merited to be further investigated as a promising anti-cancer candidate. © 2015 Elsevier Inc.


Zhang T.,Peking Union Medical College | Shen W.,Zhejiang Xianju Pharmaceutical | Liu M.,Peking Union Medical College | Zhang R.,Peking Union Medical College | And 5 more authors.
European Journal of Medicinal Chemistry | Year: 2015

A series of novel fluoroquinolone derivatives containing an 3-alkoxyimino-4-(cyclopropylanimo)methylpyrrolidine moiety were designed, synthesized and evaluated for their biological activity. Our results revealed that 19b2 shows good activity against MTB H37Rv ATCC 27294 (MIC: <0.25 Î1/4g/mL) and MDR-MTB 6133 clinical isolate (MIC: 0.11 Î1/4g/mL). Most of them have potent potency against Gram-positive strains, although they are generally poor active against Gram-negative strains. Especially, compounds 22b1 and 23a3 (MICs: <0.008-8 Î1/4g/mL) were found to 2-128 times more potent than ciprofloxacin and levofloxacin against all of the tested Gram-positive strains including quinolone-resistant MRSA, MRSE, Enterococcus faecium and Enterococcus faecalis © 2015 Published by Elsevier Masson SAS.


PubMed | Zhejiang Xianju Pharmaceutical and Peking Union Medical College
Type: Journal Article | Journal: Molecules (Basel, Switzerland) | Year: 2016

We report herein the design and synthesis of a series of novel 5-bromo-7-azaindolin-2-one derivatives containing a 2,4-dimethyl-1


PubMed | Zhejiang Xianju Pharmaceutical, Capital Medical University and Peking Union Medical College
Type: | Journal: European journal of medicinal chemistry | Year: 2015

A series of novel fluoroquinolone derivatives containing an 3-alkoxyimino-4-(cyclopropylanimo)methylpyrrolidine moiety were designed, synthesized and evaluated for their biological activity. Our results revealed that 19b2 shows good activity against MTB H37Rv ATCC 27294 (MIC: <0.25g/mL) and MDR-MTB 6133 clinical isolate (MIC: 0.11g/mL). Most of them have potent potency against Gram-positive strains, although they are generally poor active against Gram-negative strains. Especially, compounds 22b1 and 23a3 (MICs: <0.008-8g/mL) were found to 2-128 times more potent than ciprofloxacin and levofloxacin against all of the tested Gram-positive strains including quinolone-resistant MRSA, MRSE, Enterococcus faecium and Enterococcus faecalis.


PubMed | Fudan University and Zhejiang Xianju Pharmaceutical
Type: | Journal: Steroids | Year: 2015

Thirteen novel furoxan-based nitric oxide (NO) releasing hybrids (14a-e, 15a-e, 17b-d) of 16,17-pyrazo-annulated steroidal derivatives were synthesized and evaluated against the MDA-MB-231, HCC1806, SKOV-3, DU145, and HUVEC cell lines for their in vitro anti-proliferative activity. Most of the compounds displayed potent anti-proliferative effects. Among them, 17c exhibited the best activity with IC50 values of 20-1.4nM against four cell lines (MDA-MB-231, SKOV-3, DU145, and HUVEC), and 1.03M against a tamoxifen resistant breast cancer cell line (HCC1806). Furthermore, five compounds (14a, 15a, 17b-d) were selected to screen for VEGF inhibitory activity. Compounds 15a, 17b,c showed obviously better activity than 2-Methoxyestradiol (2-ME) on reducing levels of VEGF secreted by MDA-MB-231 cell line. In a Capillary-like Tube Formation Assay, compounds 17b,c exhibited a significant suppression of the tubule formation in the concentration of 1.75nM and 58nM, respectively. The preliminary SAR showed that steroidal scaffolds with a linker in 3-position were favorable moieties to evidently increase the bioactivities of these hybrids. Overall, these results implied that 17c merited to be further investigated as a promising anti-cancer candidate.


PubMed | Zhejiang Xianju Pharmaceutical, Capital Medical University and Peking Union Medical College
Type: Journal Article | Journal: Molecules (Basel, Switzerland) | Year: 2016

We report herein the design and synthesis of a series of novel imidazo[1,2-a]pyridine amide-cinnamamide hybrids linked via an alkyl carbon chain. All 38 new hybrids were evaluated for their antimycobacterial activity against M. tuberculosis (MTB) H37Rv ATCC 27294 using the microplate Alamar Blue assay (MABA). Although the hybrids are less active than the two reference compounds, the promising activity (MICs: 4 g/mL) of 2,6-dimethylimidazo[1,2-a]pyridine amide-cinnamamide hybrids 11e and 11k could be a good starting point to further find new lead compounds against multi-drug-resistant tuberculosis.


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