Diaryl ether: a privileged scaffold for drug and agrochemical discovery

T Chen, H Xiong, JF Yang, XL Zhu… - Journal of Agricultural …, 2020 - ACS Publications
Diaryl ether (DE) is a functional scaffold existing widely both in natural products (NPs) and
synthetic organic compounds. Statistically, DE is the second most popular and enduring …

[HTML][HTML] Late-stage modification of bioactive compounds: Improving druggability through efficient molecular editing

T Huo, X Zhao, Z Cheng, J Wei, M Zhu, X Dou… - … Pharmaceutica Sinica B, 2024 - Elsevier
Synthetic chemistry plays an indispensable role in drug discovery, contributing to hit
compounds identification, lead compounds optimization, candidate drugs preparation, and …

Synthesis and biological evaluation of curcumin inspired indole analogues as tubulin polymerization inhibitors

PVS Ramya, S Angapelly, L Guntuku, CS Digwal… - European Journal of …, 2017 - Elsevier
In our endeavour towards the development of potent cytotoxic agents, a series of some new
curcumin inspired indole analogues, in which indole and phenyl moieties are linked on …

Biocatalytic methylation and demethylation via a shuttle catalysis concept involving corrinoid proteins

JE Farnberger, N Richter, K Hiebler… - Communications …, 2018 - nature.com
Synthetically established methods for methylation of phenols and demethylation of methyl
phenyl ethers rely in general on hazardous reagents or/and harsh reaction conditions and …

Current trends in macrocyclic drug discovery and beyond-Ro5

S Alihodžić, M Bukvić, IJ Elenkov, A Hutinec… - Progress in Medicinal …, 2018 - Elsevier
This chapter will discuss the recent literature of macrocycles and drug-like property space
moving beyond the rule of five (bRo5). Trends in chemical classes that fall within this …

Design and synthesis of furyl/thineyl pyrroloquinolones based on natural alkaloid perlolyrine, lead to the discovery of potent and selective PDE5 inhibitors

H Zheng, L Li, B Sun, Y Gao, W Song, X Zhao… - European journal of …, 2018 - Elsevier
Abstract Based on perlolyrine (1), a natural alkaloid with weak PDE5 potency from the
traditional Chinese aphrodisiac plant Tribulus terrestris L., a series α-substituted tetrahydro …

Metal-free iodination of arylaldehydes for total synthesis of aristogins A–F and hernandial

F Wu, C Tang, X Li, N Li, M Liu, D Li, R Dai… - Organic & …, 2024 - pubs.rsc.org
Iodine is one of the most effective sources for iodination of aromatic compounds; however,
its electrophilicity is insufficient for direct iodination. The selection of appropriate …

Design, synthesis and biological evaluation of nitrogen-containing macrocyclic bisbibenzyl derivatives as potent anticancer agents by targeting the lysosome

B Sun, J Liu, Y Gao, H Zheng, L Li, Q Hu… - European Journal of …, 2017 - Elsevier
A series of novel nitrogen-containing macrocyclic bisbibenzyl derivatives was designed,
synthesized, and evaluated for antiproliferative activity against three anthropic cancer cell …

Discovery of furyl/thienyl β-carboline derivatives as potent and selective PDE5 inhibitors with excellent vasorelaxant effect

H Zheng, Y Wu, B Sun, C Cheng, Y Qiao… - European Journal of …, 2018 - Elsevier
Based on our previous studies and predictive docking results, furans and thiophenes were
introduced to the privileged tetrahydro-β-carboline scaffold to generate more potent and …

Design, synthesis and bioevaluation of antitubulin agents carrying diaryl-5, 5-fused-heterocycle scaffold

Q Xu, M Sun, Z Bai, Y Wang, Y Wu, H Tian… - European Journal of …, 2017 - Elsevier
Abstract A series of 3, 6-diaryl-1H-pyrazolo [5, 1-c][1, 2, 4] triazoles (I) and 3, 6-diaryl-[1, 2, 4]
triazolo [3, 4-b][1, 3, 4] thiadiazoles (II) as antitubulin agents were designed, synthesized and …