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

Emerging therapeutic strategies in cancer therapy by HDAC inhibition as the chemotherapeutic potent and epigenetic regulator DOI

Dipanjan Karati,

Swarupananda Mukherjee, Souvik Roy

et al.

Medical Oncology, Journal Year: 2024, Volume and Issue: 41(4)

Published: March 5, 2024

Language: Английский

Citations

12
Oxadiazole derivatives: Histone deacetylase inhibitors in anticancer therapy and drug discovery DOI Creative Commons
Balaji Wamanrao Matore, Purusottam Banjare, Tanmoy Guria

et al.

European Journal of Medicinal Chemistry Reports, Journal Year: 2022, Volume and Issue: 5, P. 100058 - 100058

Published: May 23, 2022

Heterocycles are being playing an important role in cancer treatment for years. Currently, a number of anticancer agents available on market, but concerns such as less effectiveness, drug resistance, adverse effects, and non-selectivity create urgent need the development newer highly potent with fewer side effects. Among heterocycles, oxadiazole is great interest recent era due to their potential activity. Structurally, five-member heterocyclic ring that contains one oxygen two nitrogen heteroatom. The mechanism cell suppression involve inhibition different growth factors enzymes including histone deacetylase (HDAC), thymidylate synthase (TS), vascular endothelial factor (VEGF), glycogen kinase-3 (GSK), epidermal (EGF), etc. HDAC considered target therapy discovery. inhibitors act by promoting acetylation histones, regulate cause death pathways, like apoptosis, differentiation, cycle arrest DNA repair, up-regulation or reactivation silenced tumor suppressors, down regulation factors. Recently, five drugs namely Vorinostat (SAHA), Romidepsin (FK-228), Belinostat (PXD-101), Panobinostat (LBH-589), Chidamide have been granted US/Chinese FDA several queue clinical trials. focused area this review summarize current status, chemistry, structure activity relationship, action, therapeutic various derivatives novel inhibiting enzymes. Finally, we highlighted future prospects agents.

Language: Английский

Citations

22
Synthesis, Anticancer Activity and Computational Docking Techniques of Some Novel Derivatives Based on Indole Bearing Oxadiazole–Triazole Moieties DOI
Gopalarao Gogisetti, Tejeswara Rao Allaka,

Umamaheswararao Kanna

et al.

Russian Journal of Bioorganic Chemistry, Journal Year: 2023, Volume and Issue: 49(3), P. 629 - 644

Published: May 11, 2023

Language: Английский

Citations

10
Technologies of targeting histone deacetylase in drug discovery: Current progress and emerging prospects DOI

Jinxiao Ru,

Yuxi Wang, Zijia Li

et al.

European Journal of Medicinal Chemistry, Journal Year: 2023, Volume and Issue: 261, P. 115800 - 115800

Published: Sept. 9, 2023

Language: Английский

Citations

10
Exploring β-carboline hybrids and their derivatives: A review on synthesis and anticancer efficiency DOI

Nur Fatihah Sulaiman,

Siti Zafirah Zulkifli, Aimi Suhaily Saaidin

et al.

European Journal of Medicinal Chemistry, Journal Year: 2025, Volume and Issue: 288, P. 117412 - 117412

Published: Feb. 18, 2025

Language: Английский

Citations

0
Design and Synthesis of Riluzole-Ciprofloxacin Hybrids as Highly Selective Mst3 Inhibitors for Cancer Treatment DOI
Deping Li,

Shuoqi Huang,

Jinjin Lai

et al.

Published: Jan. 1, 2025

Language: Английский

Citations

0
Vorinostat, a potential hormetin, extends lifespan and enhances stress resistance via the SKN-1 pathway in Caenorhabditis elegans DOI
Shuai Huang,

Hang Shi,

Zhengxuan Shi

et al.

Biogerontology, Journal Year: 2025, Volume and Issue: 26(3)

Published: April 25, 2025

Language: Английский

Citations

0
Design, synthesis and biological evaluation of novel substituted indazole-1,2,3-triazolyl-1,3,4-oxadiazoles: Antimicrobial activity evaluation and docking study DOI Creative Commons
Ananda Kumar Dunga, Tejeswara Rao Allaka,

Yugandhar Kethavarapu

et al.

Results in Chemistry, Journal Year: 2022, Volume and Issue: 4, P. 100605 - 100605

Published: Jan. 1, 2022

A novel series of dual 1,2,3–triazole and 1,3,4–oxadiazole heterocyclic compounds linked to indazole were designed efficiently synthesized using 3-bromo-1H-indazole as potential antimicrobial agents. All the characterized by their proton, carbon nuclear magnetic resonance, infrared, mass spectral data, elemental analysis. The final 9a–m evaluated in vitro activity against Gram–negative microorganism E. coli, Gram–positive microorganisms B. subtilis, S. pneumoniae, aureus antifungal strains A. fumigates, C. albicans. From biological screening, we surprised find that most have significant inhibitory particular heterocycles 9b, 9c, 9h, 9i, 9j showed outstanding antibacterial bacteria pneumoniae with MICs 5.4 ± 0.02, 5.8 0.03, 8.0 0.04, 4.0 7.8 0.01 µg/mL respectively, when compared ampicillin [MIC = 9.1 µg/mL]. Final prepared scaffolds 9h acquiring highest drug scores ΔG –7.78, –8.34 Kcal/mol amino acids residues Arg171 (O…H: 1.934), Lys20 (N…H: 1.951), Arg265 2.080), ArgA:171 (2.740), ArgA:265 (1.874), TyrA:248 (1.973), Ser19 (H…O: 2.048), Tyr248 1.570), 1.976), Arg46 1.059) ArgA:45 (O…H, 2.94 Å) respectively.

Language: Английский

Citations

16
Synthesis, Anticancer Activity and Molecular Docking Studies of Novel N-Mannich Bases of 1,3,4-Oxadiazole Based on 4,6-Dimethylpyridine Scaffold DOI Open Access
Małgorzata Strzelecka,

Teresa Glomb,

Małgorzata Drąg‐Zalesińska

et al.

International Journal of Molecular Sciences, Journal Year: 2022, Volume and Issue: 23(19), P. 11173 - 11173

Published: Sept. 22, 2022

Cancer is one of the greatest challenges in modern medicine today. Difficult and long-term treatment, many side effects drugs used growing resistance to treatment neoplastic cells necessitate new approaches therapy. A very promising targeted therapy based on direct impact only cancer cells. As a continuation our research biologically active molecules, we report herein design, synthesis anticancer evaluation series N-Mannich-base-type hybrid compounds containing morfoline or different substituted piperazines moieties, 1,3,4-oxadiazole ring 4,6-dimethylpyridine core. All were tested for their potential cytotoxicity against five human cell lines, A375, C32, SNB-19, MCF-7/WT MCF-7/DX. Two N-Mannich bases (compounds 5 6) further evaluated growth inhibition melanoma (A375 C32), normal (HaCaT) lines using clonogenic assay population doubling time test. The apoptosis was determined with neutral version comet assay. confocal microscopy method enabled visualization F-actin reorganization. obtained results demonstrated that 6 have cytotoxic proapoptotic are capable inducing depolarization dose-dependent manner. Moreover, computational chemistry approaches, molecular docking electrostatic employed study non-covalent interactions investigated four receptors. It found all examined molecules exhibit similar binding affinity respect chosen reference drugs.

Language: Английский

Citations

13
Hydroxamic acid hybrids: Histone deacetylase inhibitors with anticancer therapeutic potency DOI
Yuan Jiang Pan,

Haodong Hou,

Bo Zhou

et al.

European Journal of Medicinal Chemistry, Journal Year: 2023, Volume and Issue: 262, P. 115879 - 115879

Published: Oct. 18, 2023

Language: Английский

Citations

8