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Bioorganic Chemistry
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#1Rajesh Kumar Sharma (BHU: Banaras Hindu University)H-Index: 15
#2Vineeta Singh (Biotechnology Institute)H-Index: 3
Last. Diksha Katiyar (BHU: Banaras Hindu University)H-Index: 12
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Abstract A series of 3-amidocoumarins has been synthesized and tested in vitro for their anitimicrobial and chitinase inhibitory activities. Among these, compounds 5k, 5l, 8b–8d, 8f and 8g exhibited good antibacterial activity with MIC values in the range of 6.25–25 µg/mL against some of the tested strains while compounds 5l, 8b, 8c and 8f showed good activity against at least one or two fungal strains. Some of the assayed compounds 5d, 5k, 5l, 8b and 8c displayed significant chitinase inhibitor...
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#1Francesca Clemente (UniFI: University of Florence)
#2Camilla Matassini (UniFI: University of Florence)H-Index: 8
Last. Francesca Cardona (UniFI: University of Florence)H-Index: 28
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Abstract The enzyme glucocerebrosidase (GCase) has become an important therapeutic target due to its involvement in pathological disorders consequent to enzyme deficiency, such as the lysosomal storage Gaucher disease (GD) and the neurological Parkinson disease (PD). Pharmacological chaperones (PCs) are small compounds able to stabilize enzymes when used at sub-inhibitory concentrations, thus rescuing enzyme activity. We report the stereodivergent synthesis of trihydroxypiperidines alkylated at ...
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Abstract A new series of styrylquinolines was designed and synthesized as anticancer agents and tubulin polymerization inhibitors. The in vitro anticancer activity of the synthesized quinolines was evaluated against four human cancer cell lines including A-2780 (human ovarian carcinoma), A-2780/RCIS (cisplatin resistant human ovarian carcinoma), MCF-7 (human breast cancer cells), MCF-7/MX (mitoxantrone resistant human breast cancer cells) and normal Huvec cells. Generally, among the forty-eight ...
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#1Louise Hendrickx (Katholieke Universiteit Leuven)
#2Vladimir Dobričić (University of Belgrade)H-Index: 8
Last. Jan Tytgat (Katholieke Universiteit Leuven)H-Index: 41
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Abstract The voltage-gated potassium channel Kv1.3 is involved in multiple autoimmune diseases, such as multiple sclerosis, rheumatoid arthritis, diabetes mellitus type 1 and psoriasis. In many auto-immune diseases better treatment options are desired as existing therapies are often ineffective or become less effective over time, for which Kv1.3 inhibitors arise as promising candidates. In this study, five compounds were selected based on a 3D similarity searching methodology and subsequently sc...
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#1Isaac T. Henneh (University of Cape Coast)
#2Boshi Huang (VCU: Virginia Commonwealth University)
Last. Yan Zhang (VCU: Virginia Commonwealth University)H-Index: 18
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Abstract Two natural products, compounds 1 and 2 were isolated from the root bark of Ziziphus abyssinica for the first time and were structurally elucidated as β-amyrin and polpunonic acid, respectively. Both compounds were further subjected to an in vivo study in rats to evaluate their anti-arthritic potency. Compared to the arthritic control group, rats treated with different doses of 1 or 2 (3, 10, and 30 mg/kg) exhibited significantly higher total change in body weight as well as lower arthr...
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#1Yang Sheng Hu (Anhui Medical University)
#2Xu Han (Anhui Medical University)
Last. Jing Bo Shi (Anhui Medical University)H-Index: 8
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Abstract Paeonol has been proved to have potential anti-inflammatory activity, but its clinical application is not extensive due to the poor anti-inflammatory activity (14.74% inhibitory activity at 20 μM). In order to discover novel lead compound with high anti-inflammatory activity, series of paeonol derivatives were designed and synthesized, their anti-inflammatory activities were screened in vitro and in vivo. Structure-activity relationships (SARs) have been fully concluded, and finally (E)...
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#1Zhong-Rui Li (Zhengzhou University)H-Index: 4
#2Feng-Zhi Suo (Zhengzhou University)H-Index: 5
Last. Bin YuH-Index: 20
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Abstract Natural protoberberine alkaloids were first identified and characterized as potent, selective and cellular active lysine specific demethylase 1 (LSD1) inhibitors. Due to our study, isoquinoline-based tetracyclic scaffold was identified as the key structural element for their anti-LSD1 activity, subtle changes of substituents attached to the core structure led to dramatic changes of the activity. Among these protoberberine alkaloids, epiberberine potently inhibited LSD1 (IC50 = 0.14 ± 0....
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#1Nerella Sridhar Goud (National Institute of Mental Health and Neurosciences)H-Index: 1
#2Venkata Krishna Kanth Makani (Indian Institute of Chemical Technology)H-Index: 4
Last. Manika Pal-Bhadra (Indian Institute of Chemical Technology)H-Index: 24
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Abstract In present study, a new series of 4, 7-disubstituted coumarin derivatives (7a-y) have been synthesized as galectin-1 targeting apoptosis inducing agents and evaluated for their in vitro cytotoxic potentials against a panel of selected human cancer cell lines namely, Brest (MCF7), Ovarian (SKOV3), Prostate (PC-3 & DU145) and normal embryonic kidney (HEK293T) cells, using MTT assay. Most of the compounds exhibited potent growth inhibitory action against the treated cancer cell lines with ...
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#1Di ZhouH-Index: 4
#2Yang Li (SPU: Shenyang Pharmaceutical University)
Last. Ning LiH-Index: 16
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Abstract Vernicia montana Lour. (tung tree) is an oil-producing plant with multiple uses, especially with its great potential in biodiesel production, which was a small Asian tree of the spurge family (Euphorbiaceae) with big economic values. However, studies on small molecular compositions of V. montana are limited. As a result, seven new lignans and one new coumacrin, and 21 known lignans, were isolated from the testas of V. montana. These isolates were confirmed in the light of spectroscopic ...
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#1Parham Taslimi (Bartın University)H-Index: 31
#2Kadir Turhan (YTU: Yıldız Technical University)H-Index: 7
Last. İlhami Gülçin (Atatürk University)H-Index: 75
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Abstract In this study, using the Cu(OTf)2 catalyst, 1H-pyrazolo[1,2-b]phthalazine-5,10-dione derivative molecules were carried out in one step and with high yield (86-91%). The previously synthesized 1H-pyrazolo[1,2-b]phthalazine-5,10-dione derivative molecules, carbonic anhydrase I and II isozymes (hCA I and II), acetylcholinesterase (AChE), butyrylcholinesterase (BChE) and α-glycosidase (α-Gly) enzyme with Ki values in the range of 4.88-15.94 nM for hCA I, 7.04-20.83 nM for hCA II, 68.25-158....
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