Discovery of novel and potent tacrine derivatives as CDK2 inhibitors DOI

Yaoguang Huang,

Deping Li, Chang Xu

и другие.

New Journal of Chemistry, Год журнала: 2022, Номер 46(43), С. 20972 - 20984

Опубликована: Янв. 1, 2022

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

Язык: Английский

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

Future Medicinal Chemistry, Год журнала: 2024, Номер 16(5), С. 469 - 492

Опубликована: Янв. 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.

Язык: Английский

Процитировано

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

и другие.

Journal of Molecular Structure, Год журнала: 2024, Номер 1308, С. 137922 - 137922

Опубликована: Март 7, 2024

Язык: Английский

Процитировано

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

Renze Yang,

Jun Wu

и другие.

Frontiers in Chemistry, Год журнала: 2022, Номер 10

Опубликована: Авг. 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

Язык: Английский

Процитировано

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

и другие.

Journal of Saudi Chemical Society, Год журнала: 2023, Номер 27(4), С. 101680 - 101680

Опубликована: Июнь 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.

Язык: Английский

Процитировано

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

и другие.

Tetrahedron, Год журнала: 2022, Номер 124, С. 132979 - 132979

Опубликована: Авг. 29, 2022

Язык: Английский

Процитировано

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

Yaoguang Huang,

Wenwu Liu,

Shuoqi Huang

и другие.

Bioorganic Chemistry, Год журнала: 2022, Номер 126, С. 105870 - 105870

Опубликована: Май 21, 2022

Язык: Английский

Процитировано

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

и другие.

International Immunopharmacology, Год журнала: 2024, Номер 143, С. 113333 - 113333

Опубликована: Окт. 9, 2024

Язык: Английский

Процитировано

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

Yaoguang Huang,

Deping Li, Chang Xu

и другие.

New Journal of Chemistry, Год журнала: 2022, Номер 46(43), С. 20972 - 20984

Опубликована: Янв. 1, 2022

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

Язык: Английский

Процитировано

1