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本文引用的文献

1
Chemistry and biology of kahalalides.海兔毒素的化学与生物学
Chem Rev. 2011 May 11;111(5):3208-35. doi: 10.1021/cr100187n. Epub 2011 Apr 11.
2
5-OHKF and NorKA, depsipeptides from a Hawaiian collection of Bryopsis pennata: binding properties for NorKA to the human neuropeptide Y Y1 receptor.5-OHKF 和 NorKA，来自夏威夷 Bryopsis pennata 集落的二肽：NorKA 与人神经肽 Y Y1 受体的结合特性。
J Nat Prod. 2009 Dec;72(12):2172-6. doi: 10.1021/np900287e.
3
Structure-activity relationship of kahalalide F synthetic analogues.卡哈拉利德F合成类似物的构效关系
J Med Chem. 2008 Aug 28;51(16):4920-31. doi: 10.1021/jm8000828. Epub 2008 Aug 1.
4
Lysosome and HER3 (ErbB3) selective anticancer agent kahalalide F: semisynthetic modifications and antifungal lead-exploration studies.溶酶体和HER3（ErbB3）选择性抗癌剂kahalalide F：半合成修饰及抗真菌先导物探索研究
J Med Chem. 2007 Sep 6;50(18):4340-50. doi: 10.1021/jm061288r. Epub 2007 Aug 14.
5
Tandem mass spectrometry of kahalalides: identification of two new cyclic depsipeptides, kahalalide R and S from Elysia grandifolia.海兔毒素的串联质谱分析：从大乳头海兔中鉴定出两种新的环缩肽，海兔毒素R和S
J Mass Spectrom. 2007 Jan;42(1):70-80. doi: 10.1002/jms.1140.
6
Kahalalide derivatives from the Indian sacoglossan mollusk Elysia grandifolia.来自印度裸鳃亚目软体动物大叶海天牛的kahalalide衍生物。
J Nat Prod. 2006 Nov;69(11):1547-53. doi: 10.1021/np060172v.
7
Convergent approaches for the synthesis of the antitumoral peptide, Kahalalide F. Study of orthogonal protecting groups.合成抗肿瘤肽Kahalalide F的收敛方法。正交保护基的研究。
J Org Chem. 2006 Sep 15;71(19):7196-204. doi: 10.1021/jo060976f.
8
Kahalalide F induces necrosis-like cell death that involves depletion of ErbB3 and inhibition of Akt signaling.卡哈拉利德F诱导类似坏死的细胞死亡，这涉及ErbB3的耗竭和Akt信号传导的抑制。
Mol Pharmacol. 2005 Aug;68(2):502-10. doi: 10.1124/mol.105.011361. Epub 2005 May 20.
9
Phase I clinical and pharmacokinetic study of kahalalide F in patients with advanced androgen refractory prostate cancer.卡哈拉利德F在晚期雄激素难治性前列腺癌患者中的I期临床及药代动力学研究。
Clin Cancer Res. 2005 Mar 1;11(5):1854-62. doi: 10.1158/1078-0432.CCR-04-1534.
10
Technology evaluation: Kahalalide F, PharmaMar.技术评估：海兔毒素F， PharmaMar公司。
Curr Opin Mol Ther. 2004 Dec;6(6):657-65.

具有抗肿瘤和抗真菌活性的 kahalalide F 类似物的体外和体内评价。

In vitro and in vivo evaluation of select kahalalide F analogs with antitumor and antifungal activities.

机构信息

Department of Pharmacognosy, School of Pharmacy, The University of Mississippi, University, MS 38677, United States.

出版信息

Bioorg Med Chem. 2011 Nov 15;19(22):6628-32. doi: 10.1016/j.bmc.2011.06.050. Epub 2011 Jun 25.

DOI:10.1016/j.bmc.2011.06.050
PMID:21839640
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3523750/
Abstract

Kahalalide F (KF) and the regioisomer isoKF are novel anticancer drugs of marine origin and currently under clinical investigation. Here we report the synthesis of two new KF analogs with significant in vitro and in vivo antifungal and antitumor activities. The primary amine hydrogen of ornithine in KF has been replaced with 4-fluoro-3-methylbenzyl and morpholin-4-yl-benzyl via reductive N-alkylation. The TGI of these analogs using the NCI-60 cell line screening revealed promising results when compared to paclitaxel. The result of in vivo hollow fiber and animal toxicity assays are presented.

摘要

Kahalalide F (KF) 和其立体异构体 isoKF 是新型海洋来源抗癌药物，目前正在进行临床研究。本文报道了两种新型 KF 类似物的合成，它们具有显著的体外和体内抗真菌和抗肿瘤活性。通过还原 N-烷基化，KF 中鸟氨酸的仲胺氢被 4-氟-3-甲基苄基和吗啉-4-基苄基取代。与紫杉醇相比，这些类似物在 NCI-60 细胞系筛选中的 TGI 显示出有希望的结果。本文还介绍了体内中空纤维和动物毒性试验的结果。