Search results: 1,714 results (approx.)

1. Role of basic aminoalkyl chains in the lead optimization of indoloquinoline alkaloids.

Indoloquinoline (IQ) is an important class of naturally occurring antimalarial alkaloids, mainly represented by cryptolepine, isocryptolepine, and neocryptolepine. The IQ structural framework consists of four isomeric ring systems differing via the linkage of indole with quinoline as [3,2-b],...

Author(s) : Nuthakki, V. K.; Ramesh Mudududdla; Bharate, S. B.

Publisher : Elsevier Masson SAS, Issy-les-Moulineaux, France

Journal article : European Journal of Medicinal Chemistry 2022 Vol.227 ref.93

2. Investigation of chalcogen bioisosteric replacement in a series of heterocyclic inhibitors of tryptophan 2,3-dioxygenase.

Selenium is an underexplored element that can be used for bioisosteric replacement of lower molecular weight chalcogens such as oxygen and sulfur. More studies regarding the impact of selenium substitution in different chemical scaffolds are needed to fully grasp this element's potential. Herein,...

Author(s) : Kozlova, A.; Thabault, L.; Dauguet, N.; Deskeuvre, M.; Stroobant, V.; Pilotte, L.; Liberelle, M.; Eynde, B. van den; Frédérick, R.

Publisher : Elsevier Masson SAS, Issy-les-Moulineaux, France

Journal article : European Journal of Medicinal Chemistry 2022 Vol.227 ref.50

3. Synthesis and in vitro antitrypanosomal evaluation of novel 6-heteroarylidene-substituted quinolone derivatives.

Human African trypanosomiasis is a vector-borne tropical disease of African origin. Presently, due to human migration and climate change, the disease might present global health and economic burdens as current chemotherapy of trypanosomiasis remains a challenge due to limited existing drugs, which...

Author(s) : Angula, K. T.; Legoabe, L. J.; Swart, T.; Hoppe, H. C.; Beteck, R. M.

Publisher : Elsevier Masson SAS, Issy-les-Moulineaux, France

Journal article : European Journal of Medicinal Chemistry 2022 Vol.227 ref.39

4. Synthesis and biological evaluation of novel schisanhenol derivatives as potential hepatoprotective agents.

Twenty-one new schisanhenol derivatives were synthesized, and their hepatoprotective effects against liver injury induced by concanavalin A (Con A) were evaluated in vitro using an MTT assay. The data indicated that most derivatives exhibited equivalent or better protective activity than the...

Author(s) : Deng LuLu; Cheng ShaSha; Li Jiang; Xu XingLian; Hao XiaoJiang; Fan YanHua; Mu ShuZhen

Publisher : Elsevier Masson SAS, Issy-les-Moulineaux, France

Journal article : European Journal of Medicinal Chemistry 2022 Vol.227

5. Construction and activity evaluation of novel benzodioxane derivatives as dual-target antifungal inhibitors.

Ergosterol exert the important function in maintaining the fluidity and osmotic pressure of fungal cells, and its key biosynthesis enzymes (Squalene epoxidase, SE; 14 α-demethylase, CYP51) displayed the obvious synergistic effects. Therefore, we expected to discover the novel antifungal compounds...

Author(s) : An YunFei; Liu WenXia; Xie HongLei; Fan HaiYan; Han Jun; Sun Bin

Publisher : Elsevier Masson SAS, Issy-les-Moulineaux, France

Journal article : European Journal of Medicinal Chemistry 2022 Vol.227 ref.34

6. Heat shock protein 90 (Hsp90)/histone deacetylase (HDAC) dual inhibitors for the treatment of azoles-resistant Candida albicans.

Clinical treatment of candidiasis has suffered from increasingly severe drug resistance and limited efficacy. Thus, novel strategies to deal with drug resistance are highly desired to develop effective therapeutic agents. Herein, dual inhibition of heat shock protein 90 (Hsp90) and histone...

Author(s) : Li ChaoChen; Tu Jie; Han GuiYan; Liu Na; Sheng ChunQuan

Publisher : Elsevier Masson SAS, Issy-les-Moulineaux, France

Journal article : European Journal of Medicinal Chemistry 2022 Vol.227 ref.42

7. The total synthesis of berberine and selected analogues, and their evaluation as amyloid beta aggregation inhibitors.

The total synthesis of berberine and selected analogues. And their evaluation as amyloid β (Aβ) aggregation inhibitors is described. The key step in the synthesis, the assembly of the berberine framework, was accomplished using an intermolecular Heck reaction. Berberine analog 17 incorporating a...

Author(s) : Tajiri, M.; Yamada, R.; Hotsumi, M.; Makabe, K.; Konno, H.

Publisher : Elsevier Masson SAS, Issy-les-Moulineaux, France

Journal article : European Journal of Medicinal Chemistry 2021 Vol.215

8. Synthesis of artemisinin-piperazine-furan ether hybrids and evaluation of in vitro cytotoxic activity.

For the first time, eight novel artemisinin-piperazine-furane ether hybrids (5a-h) were efficiently synthesized and investigated for their in vitro cytotoxic activity against some human cancer and benign cells. The absolute configuration of hybrid 5c was determined by X-ray crystallographic...

Author(s) : Wei MengXue; Yu JiaYing; Liu XinXin; Li XueQiang; Zhang MengWei; Yang PeiWen; Yang JinHui

Publisher : Elsevier Masson SAS, Issy-les-Moulineaux, France

Journal article : European Journal of Medicinal Chemistry 2021 Vol.215

9. Biguanides: species with versatile therapeutic applications.

Biguanides are compounds in which two guanidine moieties are fused to form a highly conjugated system. Biguanides are highly basic and hence they are available as salts mostly hydrochloride salts, these cationic species have been found to exhibit many therapeutic properties. This review covers the...

Author(s) : Deepika Kathuria; Raul, A. D.; Pravin Wanjari; Bharatam, P. V.

Publisher : Elsevier Masson SAS, Issy-les-Moulineaux, France

Journal article : European Journal of Medicinal Chemistry 2021 Vol.219

10. Advancement of chimeric hybrid drugs to cure malaria infection: an overview with special emphasis on Endoperoxide pharmacophores.

Emergence and spread of Plasmodium falciparum resistant to artemisinin-based combination therapy has led to a situation of haste in the scientific and pharmaceutical communities. Sincere efforts are redirected towards finding alternative chemotherapeutic agents that are capable of combating...

Author(s) : Bhawana Sharma; Preeti Singh; Singh, A. K.; Awasthi, S. K.

Publisher : Elsevier Masson SAS, Issy-les-Moulineaux, France

Journal article : European Journal of Medicinal Chemistry 2021 Vol.219

11. An insight in anti-malarial potential of indole scaffold: a review.

Malaria is a major parasitic disease in tropical and sub-tropical regions. Pertaining to the sustaining resistance in malarial parasite against the available drugs, novel treatment options are the need of the hour. In this resolve recently, focus has shifted to finding the natural alternatives that ...

Author(s) : Mehak Chauhan; Anjali Saxena; Biswajit Saha

Publisher : Elsevier Masson SAS, Issy-les-Moulineaux, France

Journal article : European Journal of Medicinal Chemistry 2021 Vol.218

12. Flavonoid-triazolyl hybrids as potential anti-hepatitis C virus agents: synthesis and biological evaluation.

A series of flavonoid-triazolyl hybrids were synthesized and evaluated as novel inhibitors of hepatitis C virus (HCV). The results of anti-HCV activity assays showed that most of the synthesized derivatives at a concentration of 100 μg/mL inhibited the generation of progeny virus. Among these...

Author(s) : Zhang Han; Zheng Xin; Li JiChong; Liu QingBo; Huang XiaoXiao; Ding HuaiWei; Suzuki, R.; Muramatsu, M.; Song ShaoJiang

Publisher : Elsevier Masson SAS, Issy-les-Moulineaux, France

Journal article : European Journal of Medicinal Chemistry 2021 Vol.218

13. The giardicidal activity of lobendazole, fabomotizole, tenatoprazole and ipriflavone: a ligand-based virtual screening and in vitro study.

A ligand-based virtual screening study to search for giardicidal compounds on a 6551 ChEMBL drugs database was carried out using molecular similarity. Three fingerprints implemented in MayaChemTools with different design and validated by ROC curves, were used. Twelve compounds were retrieved from...

Author(s) : Pérez-Villanueva, J.; Yépez-Mulia, L.; Rodríguez-Villar, K.; Cortés-Benítez, F.; Palacios-Espinosa, J. F.; Soria-Arteche, O.

Publisher : Elsevier Masson SAS, Issy-les-Moulineaux, France

Journal article : European Journal of Medicinal Chemistry 2021 Vol.211

15. Recent advances of quinones as a privileged structure in drug discovery.

Privileged structures are conductive to discover novel bioactive substances because they can bind to multiple targets with high affinity. Quinones are considered to be a privileged structure and useful template for the design of new compounds with potential pharmacological activity. This article...

Author(s) : Zhang Li; Zhang GuiYing; Xu ShuJing; Song YuNing

Publisher : Elsevier Masson SAS, Issy-les-Moulineaux, France

Journal article : European Journal of Medicinal Chemistry 2021 Vol.223 ref.62

16. Camptothecin's journey from discovery to WHO essential medicine: fifty years of promise.

Nature represents a rich source of compounds used for the treatment of many diseases. Camptothecin (CPT), isolated from the bark of Camptotheca acuminata, is a cytotoxic alkaloid that attenuates cancer cell replication by inhibiting DNA topoisomerase 1. Despite its promising and wide spectrum...

Author(s) : Khaiwa, N.; Maarouf, N. R.; Darwish, M. H.; Alhamad, D. W. M.; Sebastian, A.; Hamad, M.; Omar, H. A.; Orive, G.; Al-Tel, T. H.

Publisher : Elsevier Masson SAS, Issy-les-Moulineaux, France

Journal article : European Journal of Medicinal Chemistry 2021 Vol.223 ref.82

17. Research progress of indole compounds with potential antidiabetic activity.

New types of antidiabetic agents are continually needed with diabetes becoming the epidemic in the world. Indole alkaloids play an important role in natural products owing to their variable structures and versatile biological activities like anticonvulsant, anti-inflammatory, antidiabetic,...

Author(s) : Zhu YuQian; Zhao JinRan; Luo LongBiao; Gao Yang; Bao He; Li PengFei; Zhang HaiLong

Publisher : Elsevier Masson SAS, Issy-les-Moulineaux, France

Journal article : European Journal of Medicinal Chemistry 2021 Vol.223

18. Anticancer potential of indirubins in medicinal chemistry: biological activity, structural modification, and structure-activity relationship.

Indirubin is the crucial ingredient of Danggui Longhui Wan and Qing-Dai, traditional Chinese medicine herbal formulas used for the therapy of chronic myelocytic leukemia in China for hundreds of years. Although the monomeric indirubin has been used in China for the treatment human chronic...

Author(s) : Wang HeZhen; Wang ZhiYuan; Wei ChunYong; Wang Jing; Xu YingShu; Bai GuoHui; Yao QiZheng; Zhang Lei; Chen YongZheng

Publisher : Elsevier Masson SAS, Issy-les-Moulineaux, France

Journal article : European Journal of Medicinal Chemistry 2021 Vol.223 ref.155

19. Dengue structural proteins as antiviral drug targets: current status in the drug discovery & development.

Dengue virus belongs to the class of RNA viruses and subclass of enveloped single-stranded positive-sense RNA virus. It causes dengue fever (DF), dengue hemorrhagic fever (DHF), or dengue shock syndrome (DSS), where DHF and DSS are life-threatening. Even though dengue is an age-old disease, it is...

Author(s) : Akshatha, H. S.; Pujar, G. V.; Sethu, A. K.; Meduri Bhagyalalitha; Manisha Singh

Publisher : Elsevier Masson SAS, Issy-les-Moulineaux, France

Journal article : European Journal of Medicinal Chemistry 2021 Vol.221

20. Design, synthesis, and biological evaluation of novel tetrahydroprotoberberine derivatives to reduce SREBPs expression for the treatment of hyperlipidemia.

Statins play an important role in the treatment of hyperlipidemia, but drug resistance and adverse effects greatly limits their application. To discover new lipid-lowering drugs, three different series of tetrahydroprotoberberine derivatives (THPBs) were designed and synthesized. These compounds...

Author(s) : Ge HaiXia; Zhang WeiTao; Yuan Kai; Xue HanYue; Cheng Hao; Chen WeiJiao; Xie YiShi; Zhang Jian; Xu XiaoJun; Yang Peng

Publisher : Elsevier Masson SAS, Issy-les-Moulineaux, France

Journal article : European Journal of Medicinal Chemistry 2021 Vol.221

21. A novel selective mitochondrial-targeted curcumin analog with remarkable cytotoxicity in glioma cells.

Naturally occurring polyphenol curcumin (4) or demethoxycurcumin (5) and their synthetic derivatives display promising anticancer activities . However, their further development is limited by low bioavailability and poor selectivity. Thus, a mitochondria-targeted compound 14 (DMC-TPP) was prepared...

Author(s) : Shi Lei; Gao LiLi; Cai ShiZhong; Xiong QianWei; Ma ZhouRui

Publisher : Elsevier Masson SAS, Issy-les-Moulineaux, France

Journal article : European Journal of Medicinal Chemistry 2021 Vol.221

22. A cyclic peptide inhibitor of the SARS-CoV-2 main protease.

This paper presents the design and study of a first-in-class cyclic peptide inhibitor against the SARS-CoV-2 main protease (Mpro). The cyclic peptide inhibitor is designed to mimic the conformation of a substrate at a C-terminal autolytic cleavage site of Mpro. The cyclic peptide contains a...

Author(s) : Kreutzer, A. G.; Krumberger, M.; Diessner, E. M.; Parrocha, C. M. T.; Morris, M. A.; Guaglianone, G.; Butts, C. T.; Nowick, J. S.

Publisher : Elsevier Masson SAS, Issy-les-Moulineaux, France

Journal article : European Journal of Medicinal Chemistry 2021 Vol.221 ref.70

23. Synergistic effects of curcumin and its analogs with other bioactive compounds: a comprehensive review.

Curcumin, as a natural compound, extracted from plant Curcuma longa, is abundant in the Indian subcontinent and Southeast Asia, and have been used in a diverse array of pharmacological activities. Although curcumin has some limitations like low stability and low bioavailability, it has been proved...

Author(s) : Hosseini-Zare, M. S.; Sarhadi, M.; Zarei, M.; Ramasamy Thilagavathi; Selvam, C.

Publisher : Elsevier Masson SAS, Issy-les-Moulineaux, France

Journal article : European Journal of Medicinal Chemistry 2021 Vol.210

24. Recent research progress of Uncaria spp. based on alkaloids: phytochemistry, pharmacology and structural chemistry.

Medicinal plants are well-known in affording clinically useful agents, with rich medicinal values by combining with disease targets through various mechanisms. Plant secondary metabolites as lead compounds lay the foundation for the discovery and development of new drugs in disease treatment. Genus ...

Author(s) : Qin Nan; Lu Xin; Liu YiJun; Qiao YuTing; Qu Wei; Feng Feng; Sun HaoPeng

Publisher : Elsevier Masson SAS, Issy-les-Moulineaux, France

Journal article : European Journal of Medicinal Chemistry 2021 Vol.210

25. A comprehensive review on β-lapachone: mechanisms, structural modifications, and therapeutic potentials.

β-Lapachone (β-lap, 1), an ortho-naphthoquinone natural product isolated from the lapacho tree (Tabebuia avellanedae) in many regions of South America, has received extensive attention due to various pharmacological activities, such as antitumor, anti-Trypanosoma cruzi, anti-Mycobacterium...

Author(s) : Gong QiJie; Hu JiaBao; Wang PengFei; Li Xiang; Zhang XiaoJin

Publisher : Elsevier Masson SAS, Issy-les-Moulineaux, France

Journal article : European Journal of Medicinal Chemistry 2021 Vol.210