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Structural activity relationship studies of zebra mussel antifouling and antimicrobial agents from verongid sponges.来自加勒比海海绵的斑马贻贝防污和抗菌剂的构效关系研究。
J Nat Prod. 2004 Dec;67(12):2117-20. doi: 10.1021/np040097t.
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Antineoplastic agents 491. Synthetic conversion of aaptamine to isoaaptamine, 9-demethylaaptamine, and 4-methylaaptamine.抗肿瘤药491. 海兔胺向异海兔胺、9-去甲基海兔胺和4-甲基海兔胺的合成转化。
J Org Chem. 2004 Apr 2;69(7):2251-6. doi: 10.1021/jo0300486.
3
Antineoplastic agents. 380. Isolation and X-ray crystal structure determination of isoaaptamine from the Republic of Singapore Hymeniacidon sp. and conversion to the phosphate prodrug hystatin 1.抗肿瘤药物。380. 从新加坡海鞘类动物 Hymeniacidon sp. 中分离异海兔胺并进行X射线晶体结构测定，以及将其转化为磷酸前药海兔抑素1。
J Nat Prod. 2004 Mar;67(3):506-9. doi: 10.1021/np0204592.
4
Antineoplastic agents. 499. Synthesis of hystatin 2 and related 1H-benzo[de][1,6]-naphthyridinium salts from aaptamine.抗肿瘤药。499. 从海兔胺合成抑癌蛋白2及相关的1H-苯并[de][1,6]萘啶鎓盐。
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Influence of substituent modifications on DNA binding energetics of acridine-based anticancer agents.
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Discovery of 4-benzoyl-1-[(4-methoxy-1H- pyrrolo[2,3-b]pyridin-3-yl)oxoacetyl]-2- (R)-methylpiperazine (BMS-378806): a novel HIV-1 attachment inhibitor that interferes with CD4-gp120 interactions.4-苯甲酰基-1-[(4-甲氧基-1H-吡咯并[2,3-b]吡啶-3-基)氧代乙酰基]-2-(R)-甲基哌嗪（BMS-378806）的发现：一种新型的HIV-1附着抑制剂，可干扰CD4与gp120的相互作用。
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Natural products as sources of new drugs over the period 1981-2002.1981年至2002年期间作为新药来源的天然产物。
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Marine natural products as lead anti-HIV agents.
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Synthesis of 8-methoxy-1-methyl-1H-benzo[de][1,6]naphthyridin-9-ol (Isoaaptamine) and analogues.8-甲氧基-1-甲基-1H-苯并[de][1,6]萘啶-9-醇（异海兔胺）及其类似物的合成。
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海洋天然产物异海兔胺C9位的修饰及其对HIV-1、分枝杆菌和肿瘤细胞活性的影响。

Modification at the C9 position of the marine natural product isoaaptamine and the impact on HIV-1, mycobacterial, and tumor cell activity.

作者信息

Gul Waseem, Hammond Nicholas L, Yousaf Muhammad, Bowling John J, Schinazi Raymond F, Wirtz Susan S, de Castro Andrews Garcia, Cuevas Carmen, Hamann Mark T

机构信息

Department of Pharmacognosy and the National Center for Natural Products Research (NCNPR), University of Mississippi School of Pharmacy, MS 38677, USA.

出版信息

Bioorg Med Chem. 2006 Dec 15;14(24):8495-505. doi: 10.1016/j.bmc.2006.08.042. Epub 2006 Oct 11.

DOI:10.1016/j.bmc.2006.08.042
PMID:17045480
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC4928486/
Abstract

As part of an investigation to generate optimized drug leads from marine natural pharmacophores for the treatment of neoplastic and infectious diseases, a series of novel isoaaptamine analogs were prepared by coupling acyl halides to the C9 position of isoaaptamine (2) isolated from the Aaptos sponge. This library of new semisynthetic products was evaluated for biological activity against HIV-1, Mtb, AIDS-OI, tropical parasitic diseases, and cancer. Compound 4 showed potent activity against HIV-1 (EC(50) 0.47microg/mL), compound 19 proved to possess remarkable activity against Mycobacterium intracellulare with an IC(50) and MIC value of 0.15 and 0.31microg/mL, while compounds 4 and 17 possessed anti-leishmanial activity with IC(50) values of 0.1 and 0.4microg/mL, respectively. Compounds 16 and 17 showed antimalarial activity with EC(50) values of 230 and 240ng/mL, respectively, and compound 14 exhibited an EC(50) of 0.05microM against the Leukemia cell line K-562.

摘要

作为从海洋天然药效基团生成用于治疗肿瘤和传染病的优化药物先导物研究的一部分，通过将酰卤与从Aaptos海绵中分离出的异海兔胺（2）的C9位偶联，制备了一系列新型异海兔胺类似物。对这个新的半合成产物文库进行了针对HIV-1、结核分枝杆菌、艾滋病相关机会性感染、热带寄生虫病和癌症的生物活性评估。化合物4对HIV-1显示出强效活性（EC(50) 0.47μg/mL），化合物19被证明对胞内分枝杆菌具有显著活性，IC(50)和MIC值分别为0.15和0.31μg/mL，而化合物4和17具有抗利什曼原虫活性，IC(50)值分别为0.1和0.4μg/mL。化合物16和17显示出抗疟活性，EC(50)值分别为230和240ng/mL，化合物14对白血病细胞系K-562的EC(50)为0.05μM。