All Outputs (64)

Synthesis, biological evaluation and mechanism studies of C-23 modified 23-hydroxybetulinic acid derivatives as anticancer agents (2019)
Journal Article

A series of C-23 modified 23-hydroxybetulinic acid (HBA) derivatives were synthesized and evaluated for their antiproliferative activity against a panel of cancer cell lines (A2780, A375, B16, MCF-7 and HepG2). The biological screening results showed... Read More about Synthesis, biological evaluation and mechanism studies of C-23 modified 23-hydroxybetulinic acid derivatives as anticancer agents.

Multi-target design strategies for the improved treatment of Alzheimer's disease (2019)
Journal Article

Alzheimer's disease (AD) is a multifactorial syndrome resulting in profound misery and poses a substantial burden on human health, economy, and society throughout the world. Based on the numerous AD-related targets in the disease network, multi-targe... Read More about Multi-target design strategies for the improved treatment of Alzheimer's disease.

Design, synthesis and biological evaluation of isochroman-4-one hybrids bearing piperazine moiety as antihypertensive agent candidates (2019)
Journal Article

7,8 Dihydroxy 3 methyl isochromanone 4 XJP is a polyphenolic natural product with moderate antihypertensive activity. T o obtain new agents with stronger potency and safer profile , we employed XJP and naftopidil as the lead compound s t o design and... Read More about Design, synthesis and biological evaluation of isochroman-4-one hybrids bearing piperazine moiety as antihypertensive agent candidates.

Controllable thioester-based hydrogen sulfide slow-releasing donors as cardioprotective agents (2019)
Journal Article

Hydrogen sulfide (H2S) is an important signaling molecule with promising protective effects in many physiological and pathological processes. However, the study of H2S has been impeded by the lack of appropriate H2S donors that could mimic its slow-r... Read More about Controllable thioester-based hydrogen sulfide slow-releasing donors as cardioprotective agents.

Design, synthesis and biological evaluation of pyridine-chalcone derivatives as novel microtubule-destabilizing agents (2019)
Journal Article

Further optimization of the trimethoxyphenyl scaffold of parent chalcone compound (2a) by introducing a pyridine ring afforded a series of novel pyridine-chalcone derivatives as potential anti-tubulin agents. All the target compounds were evaluated f... Read More about Design, synthesis and biological evaluation of pyridine-chalcone derivatives as novel microtubule-destabilizing agents.

Design, synthesis, and biological evaluation of truncated deguelin derivatives as Hsp90 inhibitors (2019)
Journal Article

A series of novel B and C-rings truncated deguelin derivatives have been designed and synthesized in the present study as heat shock protein 90 (Hsp90) inhibitors. The synthesized compounds exhibited micromolar antiproliferative potency toward a pane... Read More about Design, synthesis, and biological evaluation of truncated deguelin derivatives as Hsp90 inhibitors.

Discovery of novel quinoline–chalcone derivatives as potent antitumor agents with microtubule polymerization inhibitory activity (2018)
Journal Article

© 2018 American Chemical Society. A series of novel quinoline-chalcone derivatives were designed, synthesized, and evaluated for their antiproliferative activity. Among them, compound 24d exhibited the most potent activity with IC 50 values ranging... Read More about Discovery of novel quinoline–chalcone derivatives as potent antitumor agents with microtubule polymerization inhibitory activity.

Synthesis, molecular properties prediction and biological evaluation of indole-vinyl sulfone derivatives as novel tubulin polymerization inhibitors targeting the colchicine binding site (2018)
Journal Article

Twenty-two novel indole-vinyl sulfone derivatives were designed, synthesized and evaluated as tubulin polymerization inhibitors. The physicochemical and drug-likeness properties of all target compounds were predicted by Osiris calculations. All compo... Read More about Synthesis, molecular properties prediction and biological evaluation of indole-vinyl sulfone derivatives as novel tubulin polymerization inhibitors targeting the colchicine binding site.

Design, synthesis and biological evaluation of quinoline-indole derivatives as anti-tubulin agents targeting the colchicine binding site (2018)
Journal Article

A series of novel isocombretastatin A-4 (isoCA-4) analogs were designed and synthesized by replacing 3,4,5-trimethoylphenyl and isovanillin of isoCA-4 with quinoline and indole moieties, respectively. The structure activity relationships (SARs) of th... Read More about Design, synthesis and biological evaluation of quinoline-indole derivatives as anti-tubulin agents targeting the colchicine binding site.

Small molecules as inhibitors of PCSK9: current status and future challenges (2018)
Journal Article

Proprotein convertase subtilisin/kexin type 9 (PCSK9) plays an important role in regulating lipoprotein metabolism by binding to low-density lipoprotein receptors (LDLRs), leading to their degradation. LDL cholesterol (LDL-C) lowering drugs that oper... Read More about Small molecules as inhibitors of PCSK9: current status and future challenges.

Discovery of novel quinazolines as potential anti-tubulin agents occupying three zones of colchicine domain (2018)
Journal Article

Synthesis, Biological Evaluation of Fluorescent 23-Hydroxybetulinic Acid Probes, and Their Cellular Localization Studies (2018)
Journal Article

© 2018 American Chemical Society. 23-Hydroxybetulinic acid (23-HBA) is a complex lupane triterpenoid, which has attracted increasing attention as an anticancer agent. However, its detailed mechanism of anticancer action remains elusive so far. To rev... Read More about Synthesis, Biological Evaluation of Fluorescent 23-Hydroxybetulinic Acid Probes, and Their Cellular Localization Studies.

Discovery of Novel 4-Arylisochromenes as Anticancer Agents Inhibiting Tubulin Polymerization (2018)
Journal Article

Discovery of novel vinyl sulfone derivatives as anti-tumor agents with microtubule polymerization inhibitory and vascular disrupting activities (2018)
Journal Article

Vinyl sulfone or sulfoxide moieties were firstly introduced to the structure of chalcone compound by replacing the carbonyl group to afford a series of novel compounds as potential anti-tubulin agents. All of the target compounds were evaluated for t... Read More about Discovery of novel vinyl sulfone derivatives as anti-tumor agents with microtubule polymerization inhibitory and vascular disrupting activities.

Design, synthesis, biological evaluation and docking study of 4-isochromanone hybrids bearing N-benzyl pyridinium moiety as dual binding site acetylcholinesterase inhibitors (part II) (2017)
Journal Article

A series of novel 4-isochromanone compounds bearing N-benzyl pyridinium moiety were designed and synthesized as acetylcholinesterase (AChE) inhibitors. The biological evaluation showed that most of the target compounds exhibited potent inhibitory act... Read More about Design, synthesis, biological evaluation and docking study of 4-isochromanone hybrids bearing N-benzyl pyridinium moiety as dual binding site acetylcholinesterase inhibitors (part II).

Tubulin inhibitors targeting the colchicine binding site: a perspective of privileged structures (2017)
Journal Article

The vital roles of microtubule in mitosis and cell division make it an attractive target for antitumor therapy. Colchicine binding site of tubulin is one of the most important pockets that have been focused on to design tubulin-destabilizing agents.... Read More about Tubulin inhibitors targeting the colchicine binding site: a perspective of privileged structures.

6,7-seco-ent-kauranoids derived from oridonin as potential anticancer agents (2017)
Journal Article

Structurally unique 6,7-seco-ent-kaurenes, which are widely distributed in the genus Isodon, have attracted considerable attention because of their antitumor activities. Previously, a convenient conversion of commercially available oridonin (1) to 6,... Read More about 6,7-seco-ent-kauranoids derived from oridonin as potential anticancer agents.

Identification, characterization, and quantification of impurities of safinamide mesilate: Process-related impurities and degradation products (2017)
Journal Article

The characterization of process-related impurities and degradation products of safinamide mesilate (SAFM) in bulk drug and a stability-indicating HPLC method for the separation and quantification of all the impurities were investigated. Four process-... Read More about Identification, characterization, and quantification of impurities of safinamide mesilate: Process-related impurities and degradation products.

Novel hybrids of natural ?-elemene bearing isopropanolamine moieties: synthesis, enhanced anticancer profile, and improved aqueous solubility (2017)
Journal Article

A series of novel ?-elemene isopropanolamine derivatives were synthesized and evaluated for their antitumor activity. The results indicated that all of the compounds showed stronger antiproliferative activities than ?-elemene as well as improved aque... Read More about Novel hybrids of natural ?-elemene bearing isopropanolamine moieties: synthesis, enhanced anticancer profile, and improved aqueous solubility.

Discovery of novel antitumor nitric oxide-donating ?-elemene hybrids through inhibiting the PI3K/Akt pathway (2017)
Journal Article

A series of novel furoxan-based NO-donating b-elemene hybrids were designed and synthesized to improve the anticancer efficacy of natural b-elemene. The bioassay results indicated that all of the target compounds exhibited significantly improved anti... Read More about Discovery of novel antitumor nitric oxide-donating ?-elemene hybrids through inhibiting the PI3K/Akt pathway.