Zhonglei Wang

Tsinghua University | TH

Cancer, with its diversity, heterogeneity, and complexity, is a significant contributor to global morbidity, disability, and mortality, highlighting the necessity for transformative treatment approaches. Photodynamic therapy (PDT) has aroused continuous interest as a viable alternative to conventional cancer treatments that encounter drug resistanc...

The ongoing COVID-19 pandemic has resulted in millions of deaths globally, highlighting the need to develop potent prophylactic and therapeutic strategies against SARS-CoV-2. Small molecule inhibitors (remdesivir, Paxlovid, and molnupiravir) are essential complements to vaccines and play important roles in clinical treatment of SARS-CoV-2. Many adv...

GS-441524, an RNA‐dependent RNA polymerase (RdRp) inhibitor, is a 1′-CN-substituted adenine C-nucleoside analog with broad-spectrum antiviral activity. However, the low oral bioavailability of GS‐441524 poses a challenge to its anti-SARS-CoV-2 efficacy. Remdesivir, the intravenously administered version (version 1.0) of GS-441524, is the first FDA-...

In this era, broad-spectrum prodrugs with anti-SARS-CoV-2 activities are gaining considerable attention owing to their potential clinical benefits and role in combating the fast-spreading COVID-19 pandemic. The last two years have seen a surge of reports on various broad-spectrum prodrugs against SARS-CoV-2, and in in vitro studies, animal models,...

Ethnopharmacological relevance Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) infection causes coronavirus disease 2019 (COVID-19), a highly pathogenic virus that has spread rapidly across the entire world. There is a critical need to develop safe and effective drugs, especially broad-spectrum antiviral and organ protection agents in...

The COVID-19 pandemic has stimulated collaborative drug discovery efforts in academia and the industry with the aim of developing therapies and vaccines that target SARS-CoV-2. Several novel therapies have been approved and deployed in the last three years. However, their clinical application has revealed limitations due to the rapid emergence of v...

The exploration of non-toxic and cost-effective dietary components, such as epigallocatechin 3-gallate and myricetin, for health improvement and disease treatment has recently attracted substantial research attention. The recent COVID-19 pandemic has provided a unique opportunity for the investigation and identification of dietary components capabl...

Natural products play an irreplaceable role in the treatment of SARS-CoV-2 infection. Nevertheless, the underlying molecular mechanisms involved remain elusive. To better understand their potential therapeutic effects, more validation studies are needed to explore underlying mechanisms systematically. This study aims to explore the potential target...

Highly permeable targeted chemotherapy is highly desired for treating non-small cell lung cancer (NSCLC). In this study, a novel stimulus-responsive, carrier-free, and triple-combination nano-system (identified as [email protected] nanoparticles [NPs]) is developed for the systemic treatment of ALK/EGFR dual-mutant NSCLC. This nanomedicine addresse...

The devastating COVID-19 pandemic has caused more than 6 million deaths worldwide during the last 2 years. Effective therapeutic agents are greatly needed, yet promising magic bullets still do not exist. Numerous natural products (cordycepin, gallinamide A, plitidepsin, telocinobufagin, and tylophorine) have been widely studied and play a potential...

In addition, therapeutic regimens, including small-molecule inhibitors and traditional medicine, are still needed. Small-molecule inhibitors are being widely studied and play an essential function in COVID-19 treatment. Gilead's controversial drug, Veklury®, was conditionally approved by the FDA to combat the pandemic and Pfizer's oral broad-spectr...

Gelsemine is a remarkable indole alkaloid isolated from the medicinal plant Gelsemium elegans (Carolina or yellow jasmine) and demonstrates effectiveness in alleviating cognitive impairment, suggesting it could be encouraged to treat Alzheimer's disease. Gelsemine comprises seven adjoining chiral carbon centres and hexacyclic cage structures, makin...

Only very recently, the oral antiviral candidate Paxlovid™ (PF‐ 07321332 + ritonavir), developed by Pfizer Inc., raises new hopes of COVID‐19 recovery in the age of Omicron variant.8PF‐07321332, the second‐generation orally bioavailable SARS‐CoV‐2 main protease (Mpro) inhibitor developed by Pfizer Inc., is a novel molecular entity that combines the...

Aflatoxins, which are produced by Aspergillus flavus, Aspergillus nomius, and Aspergillus parasiticus, are a group of pentacyclic natural products with difuran and coumarin skeletons. They mainly include aflatoxin B1, B2, G1, G2, M1, and M2. Biologically, aflatoxins are of concern to human health as they can be present as contaminants in food produ...

Safer and more-effective drugs are urgently needed to counter infections with the highly pathogenic SARS-CoV-2, cause of the COVID-19 pandemic. Identification of efficient inhibitors to treat and prevent SARS-CoV-2 infection is a predominant focus. Encouragingly, using X-ray crystal structures of therapeutically relevant drug targets (PLpro, Mpro,...

As a public health emergency of international concern, the highly contagious coronavirus disease 2019 (COVID-19) pandemic has been identified as a severe threat to the lives of billions of individuals. Lung cancer, a malignant tumor with the highest mortality rate, has brought significant challenges to both human health and economic development. Na...

The novel and highly pathogenic severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), which causes coronavirus disease 2019 (COVID-19), has become a continued focus of global attention due to the serious threat it poses to public health. There are no specific drugs available to combat SARS-CoV-2 infection. Natural products (carolacton, homo...

Coronavirus disease 2019 (COVID-19) is caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) infection. COVID-19 is an ongoing global health crisis. Efficacious drugs against COVID-19 are not yet available. Therefore, rapid discovery of safe and efficacious agents against SARS-CoV-2 are needed urgently. Nucleoside analogs have an i...

Chirality is one of the most important attributes for its presence in a vast majority of bioactive natural products and pharmaceuticals. Asymmetric organocatalysis methods have emerged as a powerful methodology for the construction of highly enantioenriched structural skeletons of the target molecules. Due to their extensive application of organoca...

The organocatalytic enantioselective Friedel-Crafts alkylation of phloroglucinol derivatives with enals is reported, providing general access to the benzylic chiral centers shown in a variety of phloroglucinol natural products. The synthetic utility is demonstrated by the very concise asymmetric total synthesis of aflatoxins B 2 .

A direct [3+2] annulation reaction between indoles and a, b-unsaturated ketones is reported, which allows the efficient assembly of densely substituted, highly functionalized pyrrolo[1,2-a]indoles. Model reactions toward the originally assigned structure of yuremamine were also described, leading to the successful construction of the core with requ...

Artemisinin, existing in the Chinese medicinal plant Artemisia annua L., is a kind of sesquiterpenoid lactone endoperoxide. It has received extensive attention from all over the world owing to its unusual trioxane structure and potent antimalarial properties. Here we demonstrate the complete chemical synthetic pathway of artemisinin, investigated t...

A novel twin drug consisting of nicotinic acid (VB3) and quercetin tetramethyl ether (QTME) has been synthesized as an antihypertensive in a total yield of 79.2% through methylation, hydrolysis, acylation and esterification starting from rutin. The structures of synthesized compounds were elucidated by 1H-NMR, 13C-NMR and elemental analysis. The an...

Flavonoids, composed of a C6-C3-C6 backbone, are a kind of secondary metabolites of natural medicine, which widely exist in the higher plant. They have received extensive attention from all over the world and obtained rapid development owing to widespread distribution, structural complexity, active diversity, and molecular plasticity. Total synthes...