[HTML][HTML] Target-based anticancer indole derivatives and insight into structure‒activity relationship: A mechanistic review update (2018–2021)

A Dhiman, R Sharma, RK Singh - Acta Pharmaceutica Sinica B, 2022 - Elsevier
Cancer, which is the uncontrolled growth of cells, is the second leading cause of death after
heart disease. Targeting drugs, especially to specific genes and proteins involved in growth …

Indole in the target-based design of anticancer agents: A versatile scaffold with diverse mechanisms

S Dadashpour, S Emami - European journal of medicinal chemistry, 2018 - Elsevier
The indole scaffold is one of the most widespread heterocycles in the naturally occurring
and synthetic bioactive compounds including anticancer agents. Due to its biodiversity and …

Molecular interactions at the colchicine binding site in tubulin: An X-ray crystallography perspective

J Wang, DD Miller, W Li - Drug discovery today, 2022 - Elsevier
Highlights•Colchicine binding site inhibitors (CBSIs) emerge as new generations of tubulin
inhibitors.•CBSIs are less susceptible to multidrug resistance than FDA-approved tubulin …

[HTML][HTML] Colchicine-binding site inhibitors from chemistry to clinic: a review

EC McLoughlin, NM O'Boyle - Pharmaceuticals, 2020 - mdpi.com
It is over 50 years since the discovery of microtubules, and they have become one of the
most important drug targets for anti-cancer therapies. Microtubules are predominantly …

Tubulin inhibitors targeting the colchicine binding site: a perspective of privileged structures

W Li, H Sun, S Xu, Z Zhu, J Xu - Future medicinal chemistry, 2017 - Taylor & Francis
The vital roles of microtubule in mitosis and cell division make it an attractive target for
antitumor therapy. Colchicine binding site of tubulin is one of the most important pockets that …

Discovery of novel quinoline–chalcone derivatives as potent antitumor agents with microtubule polymerization inhibitory activity

W Li, F Xu, W Shuai, H Sun, H Yao, C Ma… - Journal of medicinal …, 2018 - ACS Publications
A series of novel quinoline–chalcone derivatives were designed, synthesized, and
evaluated for their antiproliferative activity. Among them, compound 24d exhibited the most …

Experimental spectroscopic, computational, hirshfeld surface, molecular docking investigations on 1H-Indole-3-Carbaldehyde

A Fatima, G Khanum, A Sharma, I Verma… - Polycyclic Aromatic …, 2023 - Taylor & Francis
Abstract 1H-Indole-3-carbaldehyde (1H-I3A) was investigated experimentally by NMR (1H-
NMR and 13 C-NMR in solution form), FT-Raman, FT-IR, UV-Visible and quantum …

Vanillin-based indolin-2-one derivative bearing a pyridyl moiety as a promising anti-breast cancer agent via anti-estrogenic activity

O Bender, I Celik, R Dogan, A Atalay, ME Shoman… - ACS …, 2023 - ACS Publications
The structure-based design introduced indoles as an essential motif in designing new
selective estrogen receptor modulators employed for treating breast cancer. Therefore, here …

Synthesis, biological evaluation, and molecular docking analysis of phenstatin based indole linked chalcones as anticancer agents and tubulin polymerization …

J Kode, J Kovvuri, B Nagaraju, S Jadhav… - Bioorganic …, 2020 - Elsevier
A library of new phenstatin based indole linked chalcone compounds (9a-z and 9aa-ad)
were designed and synthesized. Of these, compound 9a with 1-methyl, 2-and 3-methoxy …

Synthesis of novel indole-thiazolidinone hybrid structures as promising scaffold with anticancer potential

A Kryshchyshyn-Dylevych, L Radko, N Finiuk… - Bioorganic & medicinal …, 2021 - Elsevier
A series of novel indole-azolidinone hybrids has been synthesized via Knoevenagel
reaction of 5-fluoro-3-formyl-1H-indole-2-carboxylic acid methyl ester and some …