21 Result(s)
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Article
FTase inhibitors and cancer: prospects for use in targeted therapies
Farnesyltransferase (FTase) is a key enzyme that catalyzes the farnesylation of Ras protein. It is used to bind RAS protein to plasma membrane to complete signal transduction. Ras has been shown to be closely ...
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Article
Structure–activity relationship studies on Pd176252 derivatives leading to discovery of novel GRP receptor antagonist with potent anticancer activity
Gastrin-releasing peptide (GRP)/gastrin-releasing peptide receptor (GRPR) have various physiological effects, and many studies report that GRPR is a potential anticancer target. Pd176252 is a typical small-mol...
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Article
Synthesis and biological evaluation of novel 1,3-diphenylurea quinoxaline derivatives as potent anticancer agents
A series of 1,3-diphenylurea quinoxaline derivatives were synthesized and characterized by 1H, 13C NMR, and HR-ESI-MS analyses. In vitro cytotoxicity of the synthesized compounds was evaluated by MTT assay agains...
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Article
Chemical constituents from Ginkgo biloba L. male flowers and their biological activities
From the male flowers of Ginkgo biloba L., 26 compounds were isolated and identified including 7-O-(β-d-glucopyranosyloxy)-5-hydroxy-1(3H)- isobenzofuranone (1), piperoside (2), 3-(4-hydroxy-3-methoxyphenyl)propa...
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Article
Advance in biological activities of natural guaiane-type sesquiterpenes
Belonging to the terpenes family, sesquiterpenes represent a group of natural compounds with diverse skeletal types. Given their unique structural features and various functional groups, these compounds posses...
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Article
Design, synthesis, antiproliferative and antibacterial evaluation of quinazolinone derivatives
A series of novel quinazolinone derivatives bearing a disulfide bond were designed and synthesized. Their in vitro antiproliferative activities were evaluated using CCK-8 assay against SMMC-7721, Hela, A549 and M...
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Article
Synthesis, antitumor and antimicrobial evaluation of novel 1,3,4-thiadiazole derivatives bearing disulfide bond
In the present study, the synthesis of novel 1,3,4-thiadiazole derivatives bearing disulfide bond are accomplished in good yields with employing a convergent synthetic route, and their in vitro antiproliferati...
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Article
Integrated in silico–in vitro screening of ovarian cancer peroxisome proliferator-activated receptor-γ agonists against a biogenic compound library
In recent years, peroxisome proliferator-activated receptor-γ (PPARγ) activation by selective agonists has been emerged as a new and promising strategy for ovarian cancer therapy and prevention. Here, an integ...
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Article
Synthesis and biological evaluation of disulfides bearing 1,2,4-triazole moiety as antiproliferative agents
A series of novel nonsymmetrical disulfides bearing 1,2,4-triazole moiety were designed, synthesized, and evaluated for their in vitro antiproliferative activities against human cancer cell lines SMMC-7721, He...
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Article
TQ-B3203, a potent proliferation inhibitor derived from camptothecin
To develop topoisomerase I targeted drug candidates with sophisticated liposolubility, a series of novel camptothecin derivatives were synthesized through structure-based molecular hybridization and prodrug de...
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Article
Exploring the possible binding mode of trisubstituted benzimidazoles analogues in silico for novel drug designtargeting Mtb FtsZ
FtsZ, an essential cytokinesis protein, was a highly promising target for antibacterial agents. Following up the identification of trisubstituted benzimidazoles targeting Mycobacterium tuberculosis FtsZ (Mtb FtsZ...
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Article
Neuroprotective effect of bisabolangelone on hydrogen peroxide-induced neurotoxicity in SH-SY5Y cells
Bisabolangelone is the main active ingredient of Angelica polymorpha, which has the good pharmacological activities such as anti-celialgia, anti-dysmenorrhea and anti-gastralgia. In this study, the neuroprotectiv...
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Article
Design and synthesis of 5-chloro-2-hydroxy-3-triazolylbenzoic acids as HIV integrase inhibitors
A series of potential HIV-1 integrase inhibitors based on 5-chloro-2-hydroxy-3-triazolylbenzoic acid scaffold was designed and synthesized. Some of these compounds exhibit potent inhibitory activities at micro...
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Article
Synthesis and in vitro antiproliferative activity of novel benzisoselenazolone derivatives
A series of novel benzisoselenazolone derivatives bearing 1,3,4-thiadiazole moiety were designed, synthesized and evaluated for their in vitro antiproliferative activities against human cancer cell lines SMMC-...
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Article
Design and synthesis of N-hydroxytriazole-4-carboxamides as HIV integrase inhibitors
A series of N-hydroxytriazole-4-carboxamide derivatives were synthesized, and their potential HIV integrase inhibitory activities were evaluated.
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Article
Coumarin-containing aminophosphonates bridged with chiral side chain: synthesis and influence of chirality on cytotoxicity and DNA binding
A series of novel coumarin-containing α-aminophosphonates with two chiral centers were synthesized and a single-crystal structure of compound 8g (8g′, (R)-diethyl ((S)-2-(4-methyl-2-oxo-2H-chromen-7-yloxy)propana...
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Article
Vanillin derivatives as the selective small molecule inhibitors of FtsZ
A series of vanillin derivatives have been designed and synthesized and their biological activities were also evaluated as potential inhibitors of FtsZ. These compounds were assayed for antibacterial activity ...
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Article
Structure-based design, synthesis, and anticonvulsant activity of isatin-1-N-phenylacetamide derivatives
In an effort to develop the potent anticonvulsant agents, a series of novel isatin-1-N-phenylacetamide derivatives was synthesized and screened for their in vivo anticonvulsant activity against maximal electrosho...
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Article
Synthesis, biological evaluation and molecular modeling studies of Schiff bases derived from 4-methylsalicylic acid as potential immunosuppressive agents
A series of Schiff bases derived from 4-methylsalicylic acid (4a–4s) were synthesized, 14 of which (4a–4h, 4j–4l, 4n, 4q, and 4s) were reported for the first time. All the synthesized compounds were evaluated for...
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Article
Synthesis and evaluation in vitro of 1-[2-(10-dihydroartemisininoxy) ethyl]-3-phenylurea derivatives as potential agents against cancer
In order to develop potent and selective anticancer agents, a series of novel artemisinin derivatives bearing urea moiety 1a–n were facilely synthesized herein and screened for their activities in vitro against t...
