Design, Synthesis and Biological Evaluation of Novel Benzothiazole Derivatives As Selective PI3Kβ Inhibitors

Overview

Journal Molecules

Publisher MDPI

Specialty Biology

Date 2016 Jul 8

PMID 27384552

Citations 10

Authors

Shuang Cao

Ruiyuan Cao

Xialing Liu

Xiang Luo

Wu Zhong

Affiliations

Soon will be listed here.

Abstract

A novel series of PI3Kβ (Phosphatidylinositol-3-kinases beta subunit) inhibitors with the structure of benzothiazole scaffold have been designed and synthesized. All the compounds have been evaluated for inhibitory activities against PI3Kα, β, γ, δ and mTOR (Mammalian target of rapamycin). Two superior compounds have been further evaluated for the IC50 values against PI3Ks/mTOR. The most promising compound 11 displays excellent anti-proliferative activity and selectivity in multiple cancer cell lines, especially in the prostate cancer cell line. Docking studies indicate the morpholine group in 2-position of benzothiazole is necessary for the potent antitumor activity, which confirms our design is reasonable.

Citing Articles

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