CA IX/XII and VEGFR-2 inhibitors(Kafrelsheikh University)(CA IX/XII and VEGFR-2 inhibitors(Kafrelsheikh University)) - 药物靶点：CA12 x CAIX x VEGFR2_在研适应症：乳腺癌_专利_临床

概要

基本信息

药物类型

小分子化药

别名

SLC-0111 Analogues

靶点

CA12 x CAIX x VEGFR2

作用机制

CA12抑制剂(carbonic anhydrase 12 inhibitors)、CAIX抑制剂(碳酸酐酶IX抑制剂)、VEGFR2拮抗剂(血管内皮细胞生长因子受体2拮抗剂)

治疗领域

肿瘤皮肤和肌肉骨骼疾病

在研适应症

乳腺癌

非在研适应症-

原研机构

Kafrelsheikh University

在研机构

Kafrelsheikh University

非在研机构-

最高研发阶段临床前

首次获批日期-

最高研发阶段(中国)-

特殊审评-

关联

100 项与 CA IX/XII and VEGFR-2 inhibitors(Kafrelsheikh University) 相关的临床结果

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100 项与 CA IX/XII and VEGFR-2 inhibitors(Kafrelsheikh University) 相关的转化医学

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100 项与 CA IX/XII and VEGFR-2 inhibitors(Kafrelsheikh University) 相关的专利（医药）

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1

项与 CA IX/XII and VEGFR-2 inhibitors(Kafrelsheikh University) 相关的文献（医药）

2024-07-02·Future Medicinal Chemistry

Isocoumarins incorporating chalcone moieties act as isoform selective tumor-associated carbonic anhydrase inhibitors

Article

作者: Ammara, Andrea ; Degirmenci, Mustafa ; Supuran, Claudiu T ; Onyilmaz, Mehmet ; Koca, Murat

Aim: A series of isocoumarin-chalcone hybrids were prepared and assays for the inhibition of four isoforms of human carbonic anhydrase (hCA; EC 4.2.1.1), hCA I, II, IX and XII. Materials & methods: Isocoumarin-chalcone hybrids were synthesized by condensing acetyl-isocoumarin with aromatic aldehydes. They did not significantly inhibit off-target cytosolic isoforms hCA I and II (K_I >100 μM) but acted as low micromolar or submicromolar inhibitors for the tumor-associated isoforms hCA IX and XII. Results & conclusion: Our work provides insights into a new and scarcely investigated chemotype which provides interesting tumor-associated CA inhibitors, considering that some such derivatives like sulfonamide SLC-0111 are in advanced clinical trials for the management of metastatic advanced solid tumors.

100 项与 CA IX/XII and VEGFR-2 inhibitors(Kafrelsheikh University) 相关的药物交易

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