Late-stage functionalization for improving drug-like molecular properties

NJ Castellino, AP Montgomery, JJ Danon… - Chemical …, 2023 - ACS Publications
The development of late-stage functionalization (LSF) methodologies, particularly C–H
functionalization, has revolutionized the field of organic synthesis. Over the past decade …

The emergence of the C–H functionalization strategy in medicinal chemistry and drug discovery

R Jana, HM Begam, E Dinda - Chemical Communications, 2021 - pubs.rsc.org
Owing to the market competitiveness and urgent societal need, an optimum speed of drug
discovery is an important criterion for successful implementation. Despite the rapid ascent of …

Transition-metal-catalyzed silylation and borylation of C–H bonds for the synthesis and functionalization of complex molecules

IF Yu, JW Wilson, JF Hartwig - Chemical Reviews, 2023 - ACS Publications
The functionalization of C–H bonds in organic molecules containing functional groups has
been one of the holy grails of catalysis. One synthetically important approach to the diverse …

CH Borylation: A Toolbox for Molecular Diversification

S Guria, MMM Hassan, B Chattopadhyay - Organic Chemistry …, 2024 - pubs.rsc.org
Iridium-catalyzed C–H activation and borylation has become as a powerful synthetic tool in
the past few decades because of the widespread applicability and versatility of organoboron …

Marine-Derived Bisindoles for Potent Selective Cancer Drug Discovery and Development

M Xu, Z Bai, B **e, R Peng, Z Du, Y Liu, G Zhang… - Molecules, 2024 - mdpi.com
Marine-derived bisindoles exhibit structural diversity and exert anti-cancer influence through
multiple mechanisms. Comprehensive research has shown that the development success …

Enantioselective Total Syntheses of Vallesamidine and Schizozygane Alkaloids

GV Ramakrishna, Z Latif, F Romiti - Journal of the American …, 2025 - ACS Publications
A general streamlined strategy for the enantioselective total syntheses of the schizozygane
family of natural products and related alkaloid vallesamidine is described. Specifically, a …

Sequential Metal Catalysis towards 7‐Oxostaurosporine and Its Non‐Natural Septanose Analogue

K Seo, SH Jang, YH Rhee - Angewandte Chemie International …, 2022 - Wiley Online Library
We report sequential metal catalysis towards indolocarbazole glycosides. The signature
event is highlighted by i) Pd0‐catalyzed addition of indolocarbazole to alkoxyallene …

A multicomponent reaction for modular assembly of indole-fused heterocycles

J Li, H Ni, W Zhang, Z Lai, H **, L Zeng, S Cui - Chemical Science, 2024 - pubs.rsc.org
Indoles are privileged chemical entities in natural products and drug discovery. Indole-fused
heterocycles, particularly seven-membered ones, have received increasing attention due to …

Selenylation/Cyclization of 1‐(2‐(Allyloxy) aryl)‐1H‐indoles Access to Seleno‐Benzo [2, 3][1, 4] oxazepino [4, 5‐a] indole Derivatives

H Liao, M Pan, H Zhao, Y Qian, J Liu… - … Synthesis & Catalysis, 2025 - Wiley Online Library
Abstract The iron (ІІІ)‐promoted tandem cyclization of 1‐(2‐(allyloxy) aryl)‐1H‐indoles with
diselenides has been developed for the preparation of seleno‐benzo [2, 3][1, 4] oxazepino …

Effective Targeting of Epithelial Mesenchymal Transition-Driven Breast Cancer Stem Cells Using Ophiobolin A, A Natural Product

K Reisenauer - 2021 - search.proquest.com
Triple negative breast cancer (TNBC) is characterized by the lack of progesterone and
estrogen hormone receptors and lack of HER2 overexpression, resulting in limited treatment …