Venkateshwarlu R, Chinnababu B, Ramulu U, Purushotham Reddy K, Damoder Reddy M, Sowjanya P, Venkateswara Rao P, Aravind S
Department of Chemistry , Osmania University , Hyderabad , Telangana State , India-500007 . Email:
Division of Natural Product Chemistry , CSIR-IICT , Hyderabad , Telangana State , India-500007.
Medchemcomm. 2016 Dec 9;8(2):394-404. doi: 10.1039/c6md00606j. eCollection 2017 Feb 1.
Stereoselective total synthesis of (-)-kunstleramide, a cytotoxic dienamide from the bark of gamble, has been accomplished by using Keck's asymmetric allylation and Trost isomerization as key reactions. Application of the developed strategy for the synthesis of a series of amide analogues () was also reported. Furthermore, the synthesized compounds were evaluated for their anti-proliferative activities against human epithelial lung carcinoma (A549), human epithelial cervical cancer (HeLa), human breast adenocarcinoma (MCF7) and human neuroblastoma (IMR32) cell lines using the SRB assay. All the compounds show moderate anti-proliferative activity against all cell lines. Some of the piperazine derivatives () strongly inhibit the growth of breast cancer cells with IC values of 8-20 μM.
通过将凯克不对称烯丙基化反应和特罗斯特异构化反应作为关键反应，实现了对来自甘博树皮的具有细胞毒性的二烯酰胺（-）-昆斯特勒酰胺的立体选择性全合成。还报道了将所开发的策略应用于一系列酰胺类似物（）的合成。此外，使用SRB测定法评估了合成化合物对人上皮肺癌（A549）、人上皮宫颈癌（HeLa）、人乳腺腺癌（MCF7）和人神经母细胞瘤（IMR32）细胞系的抗增殖活性。所有化合物对所有细胞系均表现出中等抗增殖活性。一些哌嗪衍生物（）以8 - 20 μM的IC值强烈抑制乳腺癌细胞的生长。
