Tubulin polymerization/P-gp-IN-1 

Tubulin polymerization/P-gp-IN-1 is a Tubulin polymerization/P-gp dual inhibitor. Tubulin polymerization/P-gp-IN-1 inhibits tubulin polymerization and induces G₂/M arrest and apoptosis. Tubulin polymerization/P-gp-IN-1 reverses MDR by inhibiting P-gp efflux function. Tubulin polymerization/P-gp-IN-1 has dual functions: direct antitumor activity and reversal of P-gp-mediated Cisplatin (HY-17394) resistance. Tubulin polymerization/P-gp-IN-1 stable binds to the tubulin CBS (ΔG = −12.4 kcal/mol) and the P-gp hydrophobic lumen (ΔG = −10.8 kcal/mol). Tubulin polymerization/P-gp-IN-1 can be used for the study of drug-resistant cervical cancer^[1].

Tubulin polymerization/P-gp-IN-1 (Compound 6h) not only confers high potency in sensitive cells such as HeLa cells (IC₅₀ = 6.69 μM), CaSki cells (IC₅₀ = 7.84 μM), and SiHa cells (IC₅₀ = 16.68 μM), but also maintains nearly equivalent efficacy against the drug-resistant HeLa/DDP cell line (IC₅₀ = 7.21 μM), and shows no significant cytotoxicity against human normal cervical cells (IC₅₀ = 51.95 μM)^[1].
Tubulin polymerization/P-gp-IN-1 (4-16 μM, 24 h) decreases the levels of polymerized α- and β-tubulin, while the levels of depolymerized tubulin increase, with effects similar to colchicine (COL) but opposite to paclitaxel (PTX), and causes microtubule network contraction (especially 8 μM and 16 μM), and the cell morphology changed from spindle-shaped to round, with microtubules remaining only in the perinuclear region in HeLa and HeLa/ DDP cells^[1].
Tubulin polymerization/P-gp-IN-1 (4-16 μM, 24 h) not only induces G₂/M cell cycle arrest but also effectively triggers apoptosis and significantly suppresses in vitro migration in a concentration-dependent manner in both HeLa and HeLa/DDP cells^[1].
Tubulin polymerization/P-gp-IN-1 (0.25-1 μM, 48 h) can effectively reverse Cisplatin resistance in HeLa/DDP cells^[1].
Tubulin polymerization/P-gp-IN-1 (0.25-1 μM, 12 h) not only concentration-dependently inhibits P-gp-mediated efflux but also maintains unchanged P-gp protein levels at 1 μM in HeLa/DDP cells, and it significantly stabilizes P-gp under elevated temperatures of 61 °C^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Tubulin polymerization/P-gp-IN-1 (Compound 6h) (0-400 μM, 96 h) maintains excellent safety (0 % mortality; 8.3 % malformation) even at concentrations up to 400 μM in zebrafish embryos^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

658.62

C₃₆H₂₉F₃N₂O₇

COC1=CC=C(C=C1NC(C2=C3C=CC=CC3=NC(C4=CC(OC(F)(F)F)=CC=C4)=C2)=O)/C=C/C(C5=CC(OC)=C(C(OC)=C5)OC)=O

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• [1]. Yan T, et al. Design and synthesis of novel quinoline-chalcone derivatives as dual inhibitors of tubulin polymerization and P-glycoprotein to overcome cisplatin resistance in cervical cancer. Bioorg Chem. 2025 Oct;165:109006.  [Content Brief]