Synthesis and anticancer activity of cinnoline sulphonamides and 4-heteroyclic derivatives: Cross-coupling approach,Journal of Heterocyclic Chemistry

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Synthesis and anticancer activity of cinnoline sulphonamides and 4-heteroyclic derivatives: Cross-coupling approach
Journal of Heterocyclic Chemistry ( IF 2.0 ) Pub Date : 2024-03-31 , DOI: 10.1002/jhet.4816
Jayaprakash Rao Yerrabelly ₁ , Mohan Babu Bommagani ₁ , Hemasri Yerrabelly ₁ , Sai Charitha Mullaguri ₂ , Rama Krishna Kancha ₂

Affiliation

A series of novel cinnoline sulphonamide derivatives and 4-substuted cinnoline derivatives (13a-h, 16a-h and 17–31 total 33 analogues) were designed based on scaffold hopping techniques and evaluated for their antileukemic activity on wild type K562 as well as imatinib resistant cell lines (K562-IR1 and K562-IR2). Out of 33 analogues, five compounds (19, 22, 23, 28, and 31) exhibited potent antileukemic activity. An easy and efficient approach to synthesize numerous cinnoline derivatives by the various cross-coupling reactions of 4-chlorocinnoline has been developed and also demonstrated that metal-free cross couplings give high product yield compared with metal catalyzed cross couplings.

中文翻译：

肉桂啉磺酰胺和4-杂环衍生物的合成和抗癌活性：交叉偶联方法

基于支架跳跃技术设计了一系列新型肉桂啉磺酰胺衍生物和4-取代的肉桂啉衍生物（13a-h、16a-h和17-31共33个类似物），并评估了它们对野生型K562以及伊马替尼的抗白血病活性耐药细胞系（K562-IR1 和 K562-IR2）。在 33 种类似物中，有 5 种化合物（19、22、23、28 和 31）表现出有效的抗白血病活性。开发了一种通过 4-氯肉啉的各种交叉偶联反应合成多种肉桂啉衍生物的简单有效的方法，并且还证明与金属催化的交叉偶联相比，无金属交叉偶联具有更高的产物收率。

更新日期：2024-03-31

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