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Updated: May 2, 2026

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
Benzothiazoles exhibit broad-spectrum antitumor activity: their potency, structure-activity and structure-metabolism
Xilei Xie1, Yu Yan1, Ning Zhu1
1Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, 2A Nanwei Rd., Xicheng Dist., Beijing 100050, PR China.
Abstract:
An antitumor activity oriented benzothiazole sublibrary was constructed from a hit compound 3 via a five stepwise procedure. All target compounds were screened for their antitumor activity against 60 human cancer cell lines. Compounds 9p, 12d and 12i, showing higher potency than hit 3, were identified. Particularly, the compound 9p gave its average 50% growth inhibition (GI₅₀) at 0.38 μM. Furthermore, incubation in human liver microsome primarily proved their metabolic stability in vitro. General structure-activity and structure-metabolism relationships were both summarized, which provides information on further strategically optimization.
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