Wang, Ru Liu, Hu You, Yuan-Yuan Wang, Xin-Yu Lv, Bing-Bing Cao, Li-Qin Xue, Jia-Yu Xu, Yun-Gen Shi, Lei
Published in
Bioorganic & medicinal chemistry letters
VEGF/VEGFR-2 signaling plays a critical part in tumor angiogenesis. Inhibition of this pathway has been considered as a promising approach for cancer treatment. In this work, a series of 6,7-dimethoxy-4-anilinoquinazoline derivatives bearing diarylamide moiety were designed, synthesized and evaluated as potent inhibitors of VEGFR-2 kinase. Their in...
Lee, Yuan-E Kodama, Takeshi Win, Nwet Nwet Ki, Dae-Won Hoang, Nhat Nam Wong, Chin Piow Lae, Khine Zar Wynn Ngwe, Hla Dairi, Tohru Morita, Hiroyuki
...
Published in
Bioorganic & medicinal chemistry letters
SmltD is an ATP-dependent ligase that catalyzes the condensation of UDP-MurNAc-l-Ala and l-Glu to form UDP-MurNAc-l-Ala-l-Glu, in the newly discovered peptidoglycan biosynthesis pathway of a Gram-negative multiple-drug-resistant pathogen, Stenotrophomonas maltophilia. Phytochemical investigation of the 70% ethanol extract from Woodfordia fruticosa ...
Noguchi, Tetsuji Umezaki, Yuma Takano, Rieko Fujimoto, Teppei Domon, Yuki Kubota, Kazufumi Ueda, Kenjiro Kawase, Yumi Yabe, Koichi Yokoyama, Miki
...
Published in
Bioorganic & medicinal chemistry letters
We identified (5R)-6-methyl-5-phenyl-1,3,4,5,6,7-hexahydro-2,5-methano-2,6-benzodiazonine (DS21980956: 4-(R)) as a novel [5.2.1]bicyclic basic compound. The scaffold was inspired by fentanyl or pethidine, which possess potent analgesic activities. DS21980956 had potent analgesic activity in the mouse acetic acid writhing test or tail flick test wit...
Zheng, Chang-Bo Gao, Wen-Cong Pang, Pan-Pan Ma, Xin Peng, Li-Chun Yang, Liang Li, Xun
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Bioorganic & medicinal chemistry letters
An array of novel 7-methoxyl-2,3-disubstituted quinoxaline derivatives was designed, synthesized and their potential antihypertensive activities were examined, in an attempt to discover potent small molecules with vasorelaxant effects. The vasoactivities of these compounds on vascular tone, as well as underlying mechanisms were hereby explored. Res...
Ohte, Satoshi Yamazaki, Hiroyuki Takahashi, Ohgi Rotinsulu, Henki Wewengkang, Defny S Sumilat, Deiske A Abdjul, Delfly B Maarisit, Wilmar Kapojos, Magie M Zhang, Huiping
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Published in
Bioorganic & medicinal chemistry letters
A new unique sesquiterpene lactone, bicyclolamellolactone A (1), was isolated together with two known monocyclofarnesol-type sesquiterpenes, lamellolactones A (2) and B (3), from the Indonesian marine sponge Lamellodysidea sp. (cf. L. herbacea). The planar structure of 1 was assigned based on its spectroscopic data (1D and 2D NMR, HRESIMS, UV, and ...
Paquet-Côté, Pierre-Alexandre Alejaldre, Lorea Lapointe Verreault, Camille Gobeil, Sophie M C Lamoureux, Rosalie Bédard, Laurie Normandeau, Charles-Olivier Lemay-St-Denis, Claudèle Pelletier, Joelle N Voyer, Normand
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Published in
Bioorganic & medicinal chemistry letters
Sulfahydantoin-based molecules may provide a means to counteract antibiotic resistance, which is on the rise. These molecules may act as inhibitors of β-lactamase enzymes, which are key in some resistance mechanisms. In this paper, we report on the synthesis of 6 novel sulfahydantoin derivatives by the key reaction of chlorosulfonyl isocyanate to f...
Raphoko, Lerato A Lekgau, Karabo Lebepe, Charity M Leboho, Tlabo C Matsebatlela, Thabe M Nxumalo, Winston
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Bioorganic & medicinal chemistry letters
The study report on the synthesis of a series of novel quinoxaline-alkynyl derivatives that were evaluated for their activity against Mycobacterium tuberculosis (Mtb) H37RV strain. A total of 19 compounds bearing an alcohol, aldehyde, mesylate and ester groups on the alkynly group, and also containing a chloro and nitro groups at the 6-position, we...
Yoon, Sung-Hwa Lee, Eunhwa Cho, Duk-Yeon Ko, Hyun Myung Baek, Ha Yeon Choi, Dong-Kug Kim, Eunha Park, Ju-Young
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Bioorganic & medicinal chemistry letters
Based on our previous report that 3-morpholino-1-phenylpropan-1-one 2, one of the fluoxetine's simplified morpholino analogue, inhibited nitric oxide (NO) production, in this paper, various substituted benzene analogues with morpholine hydrochloride of 2 were synthesized and their inhibitory effects on NO production in lipopolysaccharide (LPS)-indu...
Ruan, Zheming Park, Peter K Wei, Donna Purandare, Ashok Wan, Honghe O'Malley, Daniel Stachura, Sylwia Perez, Heidi Cavallaro, Cullen L Weigelt, Carolyn A
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Published in
Bioorganic & medicinal chemistry letters
The discovery of a series of substituted diarylether compounds as retinoic acid related orphan receptor γt (RORγt) agonists is described. Compound 1 was identified from deck mining as a RORγt agonist. Hit-to-lead optimization led to the identification of lead compound 5, which possesses improved potency (10x). Extensive SAR exploration led to the i...
Ichimaru, Yoshimi Kato, Koichi Okuno, Yoshinori Yamaguchi, Yoshihiro Jin, Wanchun Fujita, Mikako Otsuka, Masami Imai, Masanori Kurosaki, Hiromasa
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Bioorganic & medicinal chemistry letters
It is necessary to design a ligand that is compatible with the target molecule to optimally use the DNA-cleaving ability of metal complexes. In this study, we synthesized an optically active dinuclear ligand, (1R,1'R,2R,2'R)-N1,N1'-(anthracene-1,8-diylbis(methylene))bis(N2,N2-bis(pyridin-2-ylmethyl)cyclohexane-1,2-diamine) (R-ABDC, 4a) and its enan...
