Discovery of novel and potent tacrine derivatives as CDK2 inhibitors DOI

Yaoguang Huang,

Deping Li, Chang Xu

et al.

New Journal of Chemistry, Journal Year: 2022, Volume and Issue: 46(43), P. 20972 - 20984

Published: Jan. 1, 2022

After optimization of the lead compound, ZLHT-7, a compound with 10-fold higher selectivity for CDK2 over CDK9, was discovered.

Language: Английский

Recent developments of hydroxamic acid hybrids as potential anti-breast cancer agents DOI Creative Commons
Xinran Cao, Yufeng Gong

Future Medicinal Chemistry, Journal Year: 2024, Volume and Issue: 16(5), P. 469 - 492

Published: Jan. 31, 2024

Histone deacetylase inhibitors not only possess favorable effects on modulating tumor microenvironment and host immune cells but also can reactivate the genes silenced due to deacetylation chromatin condensation. Hydroxamic acid hybrids as promising histone have potential address drug resistance reduce severe side associated with a single molecule their capacity simultaneously modulate multiple targets in cancer cells. Accordingly, rational design of hydroxamic may provide valuable therapeutic interventions for treatment breast cancer. This review aimed insights into vitro vivo anti-breast hybrids, together mechanisms action structure–activity relationships, covering articles published from 2020 present.

Language: Английский

Citations

2
IMesCuCl/TBHP system for aqueous oxidative amidation: Synthesis of new amide derivatives as EGFR targeting anti-breast cancer agents and computational studies DOI

Ravikumar Reddy Sagam,

Mohammad Azam, Saud I. Al–Resayes

et al.

Journal of Molecular Structure, Journal Year: 2024, Volume and Issue: 1308, P. 137922 - 137922

Published: March 7, 2024

Language: Английский

Citations

2
Comprehensive review of α-carboline alkaloids: Natural products, updated synthesis, and biological activities DOI Creative Commons
Deping Li,

Renze Yang,

Jun Wu

et al.

Frontiers in Chemistry, Journal Year: 2022, Volume and Issue: 10

Published: Aug. 26, 2022

α-carboline (9 H -pyrido[2,3- b ]indole), contains a pyridine ring fused with an indole backbone, is promising scaffold for medicinal chemistry. In recent decades, accumulating evidence shows that natural products and their derivatives possess diverse bioactivities. However, hitherto, there no comprehensive review to systematically summarize this important class of alkaloids. perspective, paper represents the first provide description α-carbolines including products, updated literature synthesis, biological activities. Their activities antitumor, anti-microbial, anti-Alzheimer’s disease, anti-atherosclerosis, antioxidant were hilighted. And targets main structure activity relationships (SARs) will be presented. Finally, challenges future directions compounds discussed. This helpful in understanding encouraging further exploration group

Language: Английский

Citations

9
In vitro evaluation of novel mefenamic acid derivatives as potential α-glucosidase and urease inhibitors: Design, synthesis, in silico and cytotoxic studies DOI Creative Commons
Saima Daud, Obaid‐ur‐Rahman Abid, Wajid Rehman

et al.

Journal of Saudi Chemical Society, Journal Year: 2023, Volume and Issue: 27(4), P. 101680 - 101680

Published: June 16, 2023

This study aim to synthesize new 1,3,4-oxadiazole derivatives incorporating mefenamic acid as promising α-glucosidase and urease inhibitors, potentially leading the treatment of postprandial hyperglycemia well H. pylori related disorders. In this regards, we have designed a series Mefenamic derivatives. The synthetic compounds were structurally elucidated through 1H NMR, 13C NMR HR-EIMS analysis. biological evaluation these against enzyme depicted some novel with potent inhibition said enzymes. All exhibited enzymes IC50 ranging from 25.81 ± 1.63–113.61 1.31 µM standard drug acarbose (IC50 = 375.82 1.76 µM) while respect possessed inhibitory potential varied between 8.04 1.01–58.18 1.03 thiourea 21.0 µM). cell viability results revealed that all found least cytotoxic. Furthermore, molecular docking studies most identify number key features involved in binding interactions inhibitors enzyme's active site.

Language: Английский

Citations

4
Synthesis of new 1,3,4-oxadiazole-1,4-benzoxazinone hybrids as tubulin polymerization inhibiting anticancer agents and their in silico studies DOI

Velaga Benarjee,

B. Saritha,

Hari Gangadhar K

et al.

Tetrahedron, Journal Year: 2022, Volume and Issue: 124, P. 132979 - 132979

Published: Aug. 29, 2022

Language: Английский

Citations

6
Discovery of novel benzofuro[3,2-b]quinoline derivatives as dual CDK2/Topo I inhibitors DOI

Yaoguang Huang,

Wenwu Liu,

Shuoqi Huang

et al.

Bioorganic Chemistry, Journal Year: 2022, Volume and Issue: 126, P. 105870 - 105870

Published: May 21, 2022

Language: Английский

Citations

5
Effect and mechanism of novel HDAC inhibitor ZDLT-1 in colorectal cancer by regulating apoptosis and inflammation DOI

Hefeng Geng,

Fang-Yuan Zheng,

Wentao Sun

et al.

International Immunopharmacology, Journal Year: 2024, Volume and Issue: 143, P. 113333 - 113333

Published: Oct. 9, 2024

Language: Английский

Citations

0
Discovery of novel and potent tacrine derivatives as CDK2 inhibitors DOI

Yaoguang Huang,

Deping Li, Chang Xu

et al.

New Journal of Chemistry, Journal Year: 2022, Volume and Issue: 46(43), P. 20972 - 20984

Published: Jan. 1, 2022

After optimization of the lead compound, ZLHT-7, a compound with 10-fold higher selectivity for CDK2 over CDK9, was discovered.

Language: Английский

Citations

1