Discovery and optimization of 4-(imidazo[1,2-a]pyrimidin-3-yl)thiazol-2-amine derivatives as novel phosphodiesterase 4 inhibitors DOI

Zongmin Wu,

Furong Zhang,

Zhexin Chen

et al.

Molecular Diversity, Journal Year: 2024, Volume and Issue: unknown

Published: Sept. 23, 2024

Language: Английский

An overview on pharmaceutical applications of phosphodiesterase enzyme 5 (PDE5) inhibitors DOI Creative Commons
Mohamed T. M. Nemr, Mohamad Abdelaziz, Mohamed Teleb

et al.

Molecular Diversity, Journal Year: 2024, Volume and Issue: unknown

Published: Nov. 27, 2024

Abstract Phosphodiesterase enzyme 5 (PDE5) inhibitors have emerged as one of the leading molecules for treatment erectile dysfunction (ED). PDE5 are categorized structurally into several classes. been a multidisciplinary endeavor that attracts attention researchers because their multiple pharmaceutical applications. Beyond action on ED, widely used in benign prostatic hypertrophy (BPH), Eisenmenger’s syndrome, Raynaud’s Disease, Intrauterine growth retardation (IUGR), Mountain sickness, Bladder pain syndrome/interstitial cystitis (BPS/IC), pulmonary arterial hypertension and type II diabetes (insulin resistance). In addition, also show promising antiproliferative activity, anti-Alzheimer COX-1/COX-2 inhibitory activity (anti-inflammatory). Pharmacokinetics, Pharmacogenetics toxicity were finally explored. The diverse therapeutic applications, high feasibility structural modification appropriate pharmacokinetic properties motivated to develop new scaffolds either under clinical trials or approved by FDA utilize them overcome some recent global concerns, such COVID-19.

Language: Английский

Citations

2
Discovery of novel 4-trifluoromethyl-2-anilinoquinoline derivatives as potential anti-cancer agents targeting SGK1 DOI

Guangcan Xu,

Lanlan Li,

Mengfan Lv

et al.

Molecular Diversity, Journal Year: 2024, Volume and Issue: unknown

Published: Aug. 9, 2024

Language: Английский

Citations

1
Synthesis, biological activities and mechanistic studies of C20-ketone pachysandra alkaloids as anti-hepatocellular carcinoma agents DOI

Jinfeng Zhao,

Jing Bai,

Xiang Yu

et al.

Molecular Diversity, Journal Year: 2024, Volume and Issue: unknown

Published: Aug. 19, 2024

Language: Английский

Citations

1
New chalcone incorporated structurally modified pyridine‐pyrimidine derivatives as anticancer agents: Their design, synthesis, and in‐vitro evaluation DOI

Swarupa Ketha,

Chithaluri Sudhakar,

Shashikala Kethireddy

et al.

Chemistry & Biodiversity, Journal Year: 2024, Volume and Issue: 21(12)

Published: Aug. 23, 2024

Abstract Chalcone‐incorporated pyridine‐pyrimidines i.e. derivatives of (5‐(6‐(pyrimidin‐5‐yl)pyridin‐3‐yl)thiophen‐2‐yl)prop‐2‐en‐1‐one were synthesized and their structures confirmed by analytical techniques. In addition, all the examined for capacity to fight against cancer towards four cell lines, including breast (MCF‐7), prostate (DU‐145 PC3), lung (A549) utilizing MTT technique clinically used chemotherapy medication, etoposide serving as a positive reference. All these results expressed in IC 50 μM, values compounds are compared with reference drug, showing ranging from 1.97±0.45 μM 3.08±0.135 μM. Among those, few 10(a–e ) demonstrated strong activities corresponding lines.

Language: Английский

Citations

0
Discovery and optimization of 4-(imidazo[1,2-a]pyrimidin-3-yl)thiazol-2-amine derivatives as novel phosphodiesterase 4 inhibitors DOI

Zongmin Wu,

Furong Zhang,

Zhexin Chen

et al.

Molecular Diversity, Journal Year: 2024, Volume and Issue: unknown

Published: Sept. 23, 2024

Language: Английский

Citations

0