Related Experiment Video
Updated: Jun 6, 2026

Facile Preparation of 4-Substituted Quinazoline Derivatives
Published on: February 15, 2016
Novel bifunctional alkylating agents, 5,10-dihydropyrrolo[1,2-b]isoquinoline derivatives, synthesis and biological
Ravi Chaniyara1, Naval Kapuriya, Huajin Dong
1Institute of Biomedical Sciences, Academia Sinica, Taipei 11529, Taiwan.
Abstract:
A series of linear pyrrolo[1,2-b]isoquinoline derivatives was synthesized for antitumor evaluation. The preliminary antitumor studies reveal that both bis(hydroxymethyl) and their bis(alkylcarbamate) derivatives show significant antitumor activity in inhibiting various human tumor cell growth in vitro. 1,2-Bis(hydroxymethyl)-3-methyl-5,10-dihydropyrrolo[1,2-b]isoquinoline (20a) was selected for antitumor studies in animal models. The results show that this agent can induce complete tumor remission or significant suppression in nude mice bearing human breast (MX-1) xenograft and ovarian (SK-OV-3) xenografts, respectively. Alkaline agarose gel shifting assay showed that 20a is able to cross-link with DNA. Studies on the cell cycle inhibition revealed that this agent induces cell arrest at G2/M phase. The results warrant further antitumor investigation against other human tumor growth in animal models.
Related Concept Videos
Inhibitors of Bacterial DNA Synthesis
Basicity of Heterocyclic Aromatic Amines
ortho–para-Directing Activators: –CH3, –OH, –⁠NH2, –OCH3
Aryldiazonium Salts to Azo Dyes: Diazo Coupling
Indirect-Acting Cholinergic Agonists: Chemistry and Structure-Activity Relationship
Reversible inhibitors display short to medium durations of action. Short-acting agents include simple alcohols with...
Five-Membered Heterocyclic Aromatic Compounds: Overview

