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August 6, 2024Journal of Medicinal Chemistry

Discovery of Indolo[3,2-c]isoquinoline Derivatives as Novel Top1/2 Dual Inhibitors with Orally Efficacious Antitumor Activity and Low Toxicity

Bichuan Wang Shanchao Wu Shuolei Jia Xiu-Qin Ruan Chunquan Sheng Qingfa Zhou

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Abstract

Topoisomerase (Top) inhibitors used in clinical cancer treatments are limited because of their toxicity and severe side effects. Noteworthily, Top1/2 dual inhibitors overcome the compensatory effect between Top1 and 2 inhibitors to exhibit stronger antitumor efficacies. In this study, a series of indolo[3,2-

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Wang et al. (2024) studied this question.

synapsesocial.com/papers/68e5d467b6db64358756a0c0 https://doi.org/10.1021/acs.jmedchem.4c00982

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Synapse has enriched 5 closely related papers on similar clinical questions. Consider them for comparative context:

1Discovery of cytotoxic indolo[1,2-<i>c</i>]quinazoline derivatives through scaffold-based design2025
2Synthesis, Biological Evaluation, and Theoretical Study of Indenoquinolinylphosphine Oxide Derivatives as Topoisomerase 1 Inhibitors and Antiproliferative AgentsOriginal Research · 2026
3New 1,3,4‒oxadiazole Quinazolines as Potential Anticancer Agents: Design, Synthesis, Biological Evaluation, and In silico Studies2024
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5Synthesis and Structure-Activity Relationship of Methyl-Substituted Indolo[2,3-b]quinolines: Novel Cytotoxic, DNA Topoisomerase II InhibitorsIn Vitro Study · 1994 · 202 citations

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Discovery of DNA Topoisomerase I Inhibitors with Low-Cytotoxicity Based on Virtual Screening from Natural Products2017
Design, Synthesis, and Investigation of the Pharmacokinetics and Anticancer Activities of Indenoisoquinoline Derivatives That Stabilize the G-Quadruplex in the <i>MYC</i> Promoter and Inhibit Topoisomerase I2024
Antiproliferative Activity, DNA/HSA Interactions and Human Topoisomerase Inhibition Evaluations of Indole-Thiazolidinone Derivatives: Are Two Indole Rings Better than One?2026

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